In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary m...In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary modes of treatment. CurCousin<sup>®</sup> is a nutritional ingredient containing bioactive Calebin A, (analog of Curcumin) with self-affirmed GRAS status. CurCousin<sup>®</sup> has been a clinically studied dietary supplement ingredient with a positive impact on body weight, lipid levels and metabolic health. Bioenhancers play an important role in increasing the bioavailability of the active in turn enhancing efficacy as well as reducing the dosage required to achieve the therapeutic effect. This study investigated the possible pharmacokinetic interaction between CurCousin<sup>®</sup> at two different doses (2.25 and 4.5 mg/kg) in the presence and absence of BioPerine<sup>®</sup> (0.27 mg/kg), a natural bioenhancer in Sprague-Dawley rats. The results revealed that the addition of BioPerine<sup>®</sup> into CurCousin<sup>®</sup> (2.25 mg/kg) half the dose when administered enhances the bioavailability and was equipotent to CurCousin<sup>®</sup> (4.5 mg/kg) double the dose without BioPerine<sup>®</sup>. Thus, leading to future clinical studies to evaluate its improved pharmacological efficacy as well as reduced therapeutic dosage.展开更多
Taxifolin loaded zein-caseinate nanoparticles(TZP)were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the rat.The formulations of TZP were optimized...Taxifolin loaded zein-caseinate nanoparticles(TZP)were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the rat.The formulations of TZP were optimized.With mass ratio of 1:1:2 between taxifolin,zein and sodium caseinate,the particle size andζpotential of TZP were(168.74±0.35)nm and−(57.67±0.25)mV,while the encapsulation and loading efficiency of taxifolin were(85.83±0.89)%and(17.11±0.88)%,respectively.After freeze-drying,TZP exhibited excellent redispersibility in water without aggregation.Physicochemical characterization showed that taxifolin existed in amorphous form in TZP and its interaction with the protein was observed.After encapsulating in TZP,the excellent dispersion of taxifolin in water signifi cantly improve its diffusion velocity through a semipermeable membrane.After oral administration,taxifolin and its 5 metabolites were identifi ed in rat plasma by ultra high performance liquid chromatography(UPLC)with quadrupole time-of-flight mass spectrometry(UPLC-QTOF-MS).The dynamic variation of taxifolin and its metabolites in plasma were then quantifi ed by UPLC with a triple-quadrupole typemass spectroscopy(UPLC-QqQ-MS/MS).A pharmacokinetic study showed that the bioavailability of taxifolin increased from 0.35%to 0.52%through TZP fabrication.The plasma concentration of taxifolin glucuronide and methylated taxifolin glucuronide was much higher than taxifolin.Glucuronidation was the dominating metabolism pathway of taxifolin in vivo.展开更多
Iron deficiency anemia(IDA)is a major global health problem.Tegillarca granosa has been considered as an excellent source of iron given its high content of iron-binding protein,ferritin.The aim of the present study wa...Iron deficiency anemia(IDA)is a major global health problem.Tegillarca granosa has been considered as an excellent source of iron given its high content of iron-binding protein,ferritin.The aim of the present study was to determine the physicochemical properties,protein structures,and iron uptake of ferritin extracted from T.granosa,and to evaluate the potential impacts of chitosan glycosylation on these characteristics.Based on Box-Behnken design and response surface methodology,the optimal conditions for glycosylation included a ferritin/chitosan mass ratio of 4:1,a pH of 5.5,a reaction time of 10 min,and a reaction temperature of 50℃.Glycosylation caused decreased surface hydrophobicity and elevated water-holding capacity of ferritin due to the introduction of hydrophilic groups.Additionally,glycosylation improved antioxidant capacity of ferritin by 20.69%–189.66%,likely owing to the protons donated by saccharide moiety to terminate free radical chain reaction.The in vitro digestibility of ferritin was elevated by 22.56%–104.85%after glycosylation,which could be associated with lessβ-sheet content in secondary structure that made the glycosylated protein less resistant to enzymatic digestion.The results of the iron bioavailability in Caco-2 cells revealed that ferritin(78.85–231.77 ngmg^(−1))exhibited better iron bioavailability than FeSO4(51.48–114.37 ngmg^(−1))and the values were further elevated by glycosylation with chitosan(296.23–358.20 ngmg^(−1)),which may be related to the physicochemical properties of ferritin via glycosylation modification.These results provide a basis for the development of T.granosa derived ferritin and its glycosylated products,and can promote the utilization of aquatic resources.展开更多
Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility...Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE.展开更多
Nanocrystals,a carrier-free colloidal delivery system in nano-sized range,is an interesting approach for poorly soluble drugs.Nanocrystals provide special features including enhancement of saturation solubility,dissol...Nanocrystals,a carrier-free colloidal delivery system in nano-sized range,is an interesting approach for poorly soluble drugs.Nanocrystals provide special features including enhancement of saturation solubility,dissolution velocity and adhesiveness to surface/cell membranes.Several strategies are applied for nanocrystals production including precipitation,milling,high pressure homogenization and combination methods such as Nano-Edge^(TM),SmartCrystal and Precipitation-lyophilization-homogenization(PLH)technology.For oral administration,many publications reported useful advantages of nanocrystals to improve in vivo performances i.e.pharmacokinetics,pharmacodynamics,safety and targeted delivery which were discussed in this review.Additionally,transformation of nanocrystals to final formulations and future trends of nanocrystals were also described.展开更多
Andrographolide (AG) is the characteristic constituent of Andrographis paniculata, of the Acanthaceae family. This plant is a well-known Asian medicinal plant that is widely used in India, China, and Thailand. A monog...Andrographolide (AG) is the characteristic constituent of Andrographis paniculata, of the Acanthaceae family. This plant is a well-known Asian medicinal plant that is widely used in India, China, and Thailand. A monograph of Herba Andrographidis (Chuanxinlian) is included in the Chinese Pharmacopoeia, which reports that this decoction can “remove heat, counteract toxicity, and reduce swellings.” The numerous potential activities of AG range from anti-inflammatory to anti-diabetic action, from neuroprotection to antitumor activity, and from hepatoprotective to anti-obesity properties. However, AG has low bioavailability and poor water solubility, which can limit its distribution and accumulation in the body after administration. In addition, AG is not stable in gastrointestinal alkaline and acidic environments, and has been reported to have a very short half-life. Among the diverse strategies that have been adopted to increase AG water solubility and permeability, the technological approach is the most useful way to develop appropriate delivery systems. This review reports on published studies related to microparticles (MPs) and nanoparticles (NPs) loaded with AG. MPs based on polylactic-glycolic acid (PLGA), alginic acid, and glucan derivatives have been developed for parenteral oral and pulmonary administration, respectively. NPs include vesicles (both liposomes and niosomes);polymeric NPs (based on polyvinyl alcohol, polymerized phenylboronic acid, PLGA, human serum albumin, poly ethylcyanoacrylate, and polymeric micelles);solid lipid NPs;microemulsions and nanoemulsions;gold NPs;nanocrystals;and nanosuspensions. Improved bioavailability, target-tissue distribution, and efficacy of AG loaded in the described drug delivery systems have been reported.展开更多
The aim of this study was to improve the in vitro dissolution rate and oral bioavailability of oleanolic acid(OA), a water insoluble drug belonging to BCS class IV. Hot melt extrusion(HME) was applied to develop OA am...The aim of this study was to improve the in vitro dissolution rate and oral bioavailability of oleanolic acid(OA), a water insoluble drug belonging to BCS class IV. Hot melt extrusion(HME) was applied to develop OA amorphous solid dispersions. The characterizations of the optimal formulation were performed by differential scanning calorimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy and in vitro dissolution test.The in vivo pharmacokinetic study was conducted in rats. As a result, OA solid dispersion based on PVP VA 64(OA-PVP) was successfully prepared. In the dissolution medium containing 0.3% SDS, OA-PVP dramatically increased the releasing rate of OA compared with the physical mixture(PM-PVP) and commercial tablet. Furthermore, OA-PVP exhibited higher AUC(P < 0.05) and Cmax(P < 0.05) than PM-PVP and commercial tablet. The superior dissolution property and bioavailability of OA-PVP mainly attributed to the amorphous state of OA in PVP VA64 and the well dispersion caused by thermal melting and shearing. Overall, hot melt extrusion was an efficient strategy to enhance the dissolution rate and oral bioavailability of OA.展开更多
Background: The objective of this study was to determine the effects of supplementing Cu on growth performance, Cu metabolism and Cu-related enzyme activities of weanling pigs fed diets with two different Cu sources, ...Background: The objective of this study was to determine the effects of supplementing Cu on growth performance, Cu metabolism and Cu-related enzyme activities of weanling pigs fed diets with two different Cu sources, and to estimate optimal Cu requirements and relative bioavailability from these two sources for pigs.Methods: Weanling pigs were allocated to 14 treatments arranged factorially, including 6 added Cu levels(5, 10,20, 40, 80, 160 mg/kg), and 2 mineral sources(tribasic Cu chloride, TBCC and copper proteinate, Cu Pro), as well as one negative control(0 mg/kg added Cu level) and one maximum allowed level treatment(200 mg/kg TBCC) for the entire 38-d experiment. Growth performance, mineral status and enzyme activities were measured at the end of this study.Results: Increasing levels of Cu showed linear and quadratic responses(P < 0.01) for final BW, ADG and FCR regardless of the sources. Supplementation with TBCC(> 80 mg/kg) and Cu Pro(> 20 mg/kg) significantly decreased(P < 0.05) diarrhea incidence of weanling pigs. There were linear and quadratic increases(P < 0.01) in bile, hepatic,and intestinal Cu concentrations, fecal Cu contents, and plasma enzyme activities(alkaline phosphatase,ceruloplasmin, Cu, Zn-Superoxide dismutase(Cu/Zn SOD), and glutathione peroxidase), whereas plasma malondialdehyde decreased(P < 0.01) linearly and quadratically as dietary Cu level increased. Similarly, pigs fed Cu Pro absorbed and retained more Cu and excreted less Cu than those fed TBCC when supplemented 80 mg/kg and above. Optimal dietary Cu requirements for pigs from 28 to 66 d of age estimated based on fitted broken-line models(P < 0.05) of bile Cu, plasma Cu/Zn SOD and growth performance were 93–140 mg/kg from TBCC, and 63–98 mg/kg from Cu Pro accordingly. According to slope ratios from multiple linear regression, the bioavailability value of Cu Pro relative to TBCC(100%) was 156–263%(P < 0.01).Conclusion: The findings indicated that Cu recommendation from current NRC(5–6 mg/kg) was not sufficient to meet the high requirement of weanling pigs. Cu from Cu Pro was significantly more bioavailable to weanling pigs than TBCC in stimulating growth and enzyme activities, decreasing diarrhea frequency and fecal Cu contents to the environment.展开更多
The objective of this study was to improve the dissolution and bioavailability of silymarin(SM).Solid dispersions(SDs)were prepared using solution-enhanced dispersion by supercritical fluids(SEDS)and evaluated in vitr...The objective of this study was to improve the dissolution and bioavailability of silymarin(SM).Solid dispersions(SDs)were prepared using solution-enhanced dispersion by supercritical fluids(SEDS)and evaluated in vitro and in vivo,compared with pure SM powder.The particle sizes,stability,and contents of residual solvent of the prepared SM-SDs with SEDS and solvent evaporation(SE)were investigated.Four polymer matrix materials were evaluated for the preparation of SM-SD-SEDS,and the hydrophilic polymer,polyvinyl pyrrolidone K17,was selected with a ratio of 1:5 between SM and the polymer.Physicochemical analyses using X-ray diffraction and differential scanning calorimetry indicated that SM was dispersed in SD in an amorphous state.The optimized SM-SD-SEDS showed no loss of SM after storage for 6 months and negligible residual solvent(ethanol)was detected using gas chromatography.In vitro drug release was increased from the SM-SDSEDS,as compared with pure SM powder or SM-SD-SE.In vivo,the area under the rat plasma SM concentration-time curve and the maximum plasma SM concentration were 2.4-fold and 1.9-fold higher,respectively,after oral administration of SM-SD-SEDS as compared with an aqueous SM suspension.These results illustrated the potential of using SEDS to prepare SM-SD,further improving the biopharmaceutical properties of this compound.展开更多
Tea polyphenols(TPPs)have attracted significant research interest due to their health benefits.However,TPPs are sensitive to certain environmental and gastrointestinal conditions and their oral bioavailability was fou...Tea polyphenols(TPPs)have attracted significant research interest due to their health benefits.However,TPPs are sensitive to certain environmental and gastrointestinal conditions and their oral bioavailability was found to be very low.Delivery systems made of food-grade materials have been reported to improve the shelf-life,bioavailability and bioefficacy of TPPs.This review discusses the chemistry of TPPs;the setbacks of TPPs for application;and the strategies to counteract application limitations by rationally designing delivery systems.An overview of different formulations used to encapsulate TPPs is provided in this study,such as emulsion-based systems(liposome,nanoemulsion,double emulsion,and Pickering emulsion)and nano/microparticles-based systems(protein-based,carbohydrate-based,and bi-polymer based).In addition,the stability,bioavailability and bioactivities of encapsulated TPPs are evaluated by various in vitro and in vivo models.The current findings provide scientific insights in encapsulation approaches for the delivery of TPPs,which can be of great value to TPPs-fortified food products.Further explorations are needed for the encapsulated TPPs in terms of their applications in the real food industry as well as their biological fate and functional pathways in vivo.展开更多
Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholi...Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ‘‘label-friendly'phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.展开更多
Recently,the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines.However,many herbal drugs and herbal extracts d...Recently,the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines.However,many herbal drugs and herbal extracts despite of their impressive in-vitro findings demonstrates less or negligible in-vivo activity due to their poor lipid solubility or improper molecular size,resulting in poor absorption and hence poor bioavailability.Nowadays with the advancement in the technology,novel drug delivery systems open the door towards the development of enhancing bioavailability of herbal drug delivery systems.For last one decade many novel carriers such as liposomes,microspheres,nanoparticles,transferosomes,ethosomes,lipid based systems etc.have been reported for successful modified delivery of various herbal drugs.Many herbal compounds including quercetin,genistein,naringin,sinomenine,pipeline,glycvrrhizin and nitrile glycoside have demonstrated capability to enhance the bioavailability.The objective of this review is to summarize various available novel drug delivery technologies which have been developed for delivery of drugs(herbal),and to achieve better therapeutic response.An attempt has also been made to compile a profile on bioavailability enhancers of herbal origin with the mechanism of action(wherever reported)and studies on improvement in drug bioavailability,exhibited particularly by natural compounds.展开更多
The effects of carbonate on the exchangeability and the bioavailability of exogenous neodymium in soil were studied by 147 Nd isotopic tracer method. Exchangeable Nd was extracted by 1 mol·L -1 NaAc (pH8 2) in th...The effects of carbonate on the exchangeability and the bioavailability of exogenous neodymium in soil were studied by 147 Nd isotopic tracer method. Exchangeable Nd was extracted by 1 mol·L -1 NaAc (pH8 2) in the experiment. The results indicate that whether carbonate exists in soil or not, beyond 99% of exogenous Nd is adsorbed by soil. Low-concentration carbonate (0 8～1 6 g·kg -1 ) can reduce exchangeable Nd concentration in soil, while high-concentration carbonate (4 0 g·kg -1 ) impacts little on the exchangeable Nd concentration. In addition, carbonate of 0 8～1 6 g·kg -1 in soil can inhibit wheat seedlings to absorb Nd. However, when the carbonate concentration rises to 4 0 g·kg -1 , the inhibition will become indistinct.展开更多
Two hundred and sixty four broiler breeder hens of 32 weeks of age were distributed randomly in four dietary treatments. The dietary treatments were T0: Broiler breeder ration containing 40 ppm zinc (basal 29.8 ppm + ...Two hundred and sixty four broiler breeder hens of 32 weeks of age were distributed randomly in four dietary treatments. The dietary treatments were T0: Broiler breeder ration containing 40 ppm zinc (basal 29.8 ppm + 10.2 ppm inorganic zinc), T1: T0 + organic zinc (zinc methionine) @ 20 ppm, T2: T0 + organic zinc @ 40 ppm and T3: T0 + organic zinc @ 60 ppm. The experiment was continued from 32 to 48 weeks of age. At 48 weeks, the weight of lymphoid organs, zinc levels in organs and immunity response were determined. The faecal zinc level was determined at monthly interval. The weight lymphoid organs of different treatment groups (both organic and inorganic zinc fed groups) of the broiler breeders did not differ significantly (P > 0.05). The cellular immune response of breeder birds to PHA-P was significantly (P 0.05) higher in group T3 than the rest of treated groups. The antibody titre to SRBC differed among the treated groups. The zinc content of serum of broiler breeders of all the groups did not differ significantly (P > 0.05) in all the periods of study. Zinc content in liver and tibia of broiler breeders in different dietary treatments of zinc differed significantly (P 0.05) with higher levels were obtained on increasing zinc concentration in the diet. The zinc level in the spleen and kidney of the broiler breeders in different dietary treatments did not differ significantly (P > 0.05). The average zinc content in the faeces of broiler breeder during 35 to 43 week of age did not differ significantly (P > 0.05) among the treated groups. At 48 weeks of age, zinc content of the faeces of T3 was found to be significantly (P 0.05) higher than the rest of treated groups. Similarly, during the overall experimental period analysis, it was found that zinc levels in the faeces of T2 and T3 were significantly (P 0.05) higher than T1 and T0.展开更多
Numerous systems have been designed during the past three decades to improve bioavailability of ophthalmic drug delivery,including:ocular prodrugs and nanotechnology-based drug delivery system.The former can improve t...Numerous systems have been designed during the past three decades to improve bioavailability of ophthalmic drug delivery,including:ocular prodrugs and nanotechnology-based drug delivery system.The former can improve the efficacy of ocular drug via enhancing corneal penetration of ocular drugs,prolonging their duration of action and/or reducing the systemic side-effects,unfortunately,some characteristics of the pro-drugs,such as poorly aqueous stability,poorly aqueous solubility and severe eye irritation probably,limit their clinical practice and cannot be ignored.As we all know,nanotech-nology for ocular drug delivery can carry poorly soluble drugs,protect the encapsulated molecules from hydrolysis,control the rate of drug delivery and prolong the precorneal retention of drugs.All of these merits may solve the problems in the utilization of ocular prodrugs and increase the bioavailability of ocular drug delivery.By reviewing recent ad-vances of prodrugs and nanostructures in ocular drug delivery,this paper focus specifically on the promising prospects of nanocarriers overcoming the drawbacks of prodrugs for ophthalmic drug delivery by precorneal routes.展开更多
The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomiz...The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomized 2 way crossover study. The concentrations in plasma were determined by HPLC UV method. The main parameters of irbesartan capsules were: C max : 1.502±0.295 μg/ml, t max : 1.44±0.34 h, t 1/2 : 20.21±14.71 h, AUC 0 t : 11.087±3.443 μg/ml -1 ·h. The relative bioavailability of capsule to tablet was (101.4±28.9) %. The results of statistical analysis showed that two formulations were bioequivalent.展开更多
Objectives: Vitamin E is an important human lipophilic antioxidant and is required for many metabolic functions. A high vitamin E intake appears to favorably impact a variety of disease processes. The vitamin E intake...Objectives: Vitamin E is an important human lipophilic antioxidant and is required for many metabolic functions. A high vitamin E intake appears to favorably impact a variety of disease processes. The vitamin E intake, excluding sup-plemental intake, of the vast majority of adults is below the current recommended level. By consuming vitamin E-enriched food, it is possible to take in adequate amounts of vitamin E. Vitamin E intake from enriched foods might prevent certain diseases without the need to ingest specific vitamin E supplements. The vitamin E that is present in enriched foods has to exhibit maximal bioavailability to ensure a sufficient intake of vitamin E from one portion of fortified food. The aim of the present study was to develop an enriched food that has highly bioavailable vitamin E. Furthermore, we wanted to examine whether vitamin E bioavailability can be affected by the technological properties of fortified food. Methods: Volunteers were given test foods (cream cheese and mayonnaise) that had been fortified with 60 mg of RRR-α-tocopherol. The test foods were technologically modified and the bioavailability of RRR-α-tocopherol was determined via a short-term kinetic measurement, which was 24 h long, and a long-term kinetic measurement, which was 28 d long. The test foods were characterized with respect to matrix properties. Results: In comparison to the mayonnaise group the serum α-tocopherol area under the curve (AUC) was significantly higher in the cream cheese group, as shown in the short-term kinetic (p = 0.010) and long-term kinetic (p = 0.017) studies. Conclusions: In conclusion, RRR-α-tocopherol was more bioavailable in cream cheese than in mayonnaise in both short-term and long-term periods. Hence, food matrices affect bioavailability of RRR-α-tocopherol. Fortified foods with proven high α-tocopherol bioavailabilities could be merchandised as functional foods with diseases prevention properties.展开更多
Objective:To enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract by formulating its nanosuspension.Methods:Nanoprecipitation approach was used for the formulation of nanosuspension ...Objective:To enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract by formulating its nanosuspension.Methods:Nanoprecipitation approach was used for the formulation of nanosuspension using polysorbate-80 as a stabilizer.The formulated nanosuspension was assessed for particle size,polydispersity index,zeta potential value and for in vitro dissolution study.Oral bioavailability studies were carried out in Wistar male albino rats by administering a single dose(50 mg/kg.b.wt)of the formulated nanosuspension and coarse suspension.The storage stability of the formulated nanosuspension was determined after three months of storage at room temperature and under the refrigerated condition.Mutagenicity assay was carried out to evaluate the toxicity of the formulated nanosuspension using two mutant strains(Salmonella typhimurium TA100 and Salmonella typhimurium TA98).Results:The mean particle size of the formulated nanosuspension was 90.53 nm with polydispersity index and zeta potential values of 0.175 and-15.7 m V,respectively.Terminalia arjuna nanosuspension showed improved dissolution rate and 1.33-fold higher oral bioavailability than its coarse suspension.The formulated nanosuspension also showed better stability under the refrigerated condition and was non-mutagenic against both strains.Conclusions:Our study demonstrates that nanosuspension technology can effectively enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract.展开更多
The in vivo bioavailability of soy protein isolates and corn zein film material before and after film formation by heat/ pressure was determined. The In vitro digestibility of corn zein before and after film formation...The in vivo bioavailability of soy protein isolates and corn zein film material before and after film formation by heat/ pressure was determined. The In vitro digestibility of corn zein before and after film formation was also measured. Films were produced from anhydrous protein with 30% glycerol added using a heat-press method with no use of casting solvents or cross-linking agents. Corn zein raw and film material were ground under liquid nitrogen then digested in two enzyme-acid cocktails with free amino acid analysis before and after digestion. The protein efficiency ratio and net protein ratio were determined for both zein and soy protein using a weanling Sprague-Dawley descended rat feeding study. The In vitro digestibility study indicated that the non-heat pressed corn zein was more digestible than the heat pressed zein. However, the in vivo results indicated that corn and soy protein were equally bioavailable whether they were derived from film mixture prior to or after film formation. Both corn zein and soy protein material had lower protein efficiency ratio than the control diet. Furthermore, soy protein films materials had a higher protein efficiency ratio than corn zein.展开更多
文摘In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary modes of treatment. CurCousin<sup>®</sup> is a nutritional ingredient containing bioactive Calebin A, (analog of Curcumin) with self-affirmed GRAS status. CurCousin<sup>®</sup> has been a clinically studied dietary supplement ingredient with a positive impact on body weight, lipid levels and metabolic health. Bioenhancers play an important role in increasing the bioavailability of the active in turn enhancing efficacy as well as reducing the dosage required to achieve the therapeutic effect. This study investigated the possible pharmacokinetic interaction between CurCousin<sup>®</sup> at two different doses (2.25 and 4.5 mg/kg) in the presence and absence of BioPerine<sup>®</sup> (0.27 mg/kg), a natural bioenhancer in Sprague-Dawley rats. The results revealed that the addition of BioPerine<sup>®</sup> into CurCousin<sup>®</sup> (2.25 mg/kg) half the dose when administered enhances the bioavailability and was equipotent to CurCousin<sup>®</sup> (4.5 mg/kg) double the dose without BioPerine<sup>®</sup>. Thus, leading to future clinical studies to evaluate its improved pharmacological efficacy as well as reduced therapeutic dosage.
基金supported by the National Natural Science Foundation of China(32060541).
文摘Taxifolin loaded zein-caseinate nanoparticles(TZP)were fabricated by the anti-solvent method and were used as an oral delivery vehicle to improve their bioavailability in the rat.The formulations of TZP were optimized.With mass ratio of 1:1:2 between taxifolin,zein and sodium caseinate,the particle size andζpotential of TZP were(168.74±0.35)nm and−(57.67±0.25)mV,while the encapsulation and loading efficiency of taxifolin were(85.83±0.89)%and(17.11±0.88)%,respectively.After freeze-drying,TZP exhibited excellent redispersibility in water without aggregation.Physicochemical characterization showed that taxifolin existed in amorphous form in TZP and its interaction with the protein was observed.After encapsulating in TZP,the excellent dispersion of taxifolin in water signifi cantly improve its diffusion velocity through a semipermeable membrane.After oral administration,taxifolin and its 5 metabolites were identifi ed in rat plasma by ultra high performance liquid chromatography(UPLC)with quadrupole time-of-flight mass spectrometry(UPLC-QTOF-MS).The dynamic variation of taxifolin and its metabolites in plasma were then quantifi ed by UPLC with a triple-quadrupole typemass spectroscopy(UPLC-QqQ-MS/MS).A pharmacokinetic study showed that the bioavailability of taxifolin increased from 0.35%to 0.52%through TZP fabrication.The plasma concentration of taxifolin glucuronide and methylated taxifolin glucuronide was much higher than taxifolin.Glucuronidation was the dominating metabolism pathway of taxifolin in vivo.
基金supported by the National Key R&D Program of China(No.2018YFD0901105).
文摘Iron deficiency anemia(IDA)is a major global health problem.Tegillarca granosa has been considered as an excellent source of iron given its high content of iron-binding protein,ferritin.The aim of the present study was to determine the physicochemical properties,protein structures,and iron uptake of ferritin extracted from T.granosa,and to evaluate the potential impacts of chitosan glycosylation on these characteristics.Based on Box-Behnken design and response surface methodology,the optimal conditions for glycosylation included a ferritin/chitosan mass ratio of 4:1,a pH of 5.5,a reaction time of 10 min,and a reaction temperature of 50℃.Glycosylation caused decreased surface hydrophobicity and elevated water-holding capacity of ferritin due to the introduction of hydrophilic groups.Additionally,glycosylation improved antioxidant capacity of ferritin by 20.69%–189.66%,likely owing to the protons donated by saccharide moiety to terminate free radical chain reaction.The in vitro digestibility of ferritin was elevated by 22.56%–104.85%after glycosylation,which could be associated with lessβ-sheet content in secondary structure that made the glycosylated protein less resistant to enzymatic digestion.The results of the iron bioavailability in Caco-2 cells revealed that ferritin(78.85–231.77 ngmg^(−1))exhibited better iron bioavailability than FeSO4(51.48–114.37 ngmg^(−1))and the values were further elevated by glycosylation with chitosan(296.23–358.20 ngmg^(−1)),which may be related to the physicochemical properties of ferritin via glycosylation modification.These results provide a basis for the development of T.granosa derived ferritin and its glycosylated products,and can promote the utilization of aquatic resources.
文摘Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE.
基金the Thailand Research Fund through Thai Basic Research Grant(BRG5680020 to V.B.J.)the Royal Golden Jubilee Ph.D.Program and Mahidol。
文摘Nanocrystals,a carrier-free colloidal delivery system in nano-sized range,is an interesting approach for poorly soluble drugs.Nanocrystals provide special features including enhancement of saturation solubility,dissolution velocity and adhesiveness to surface/cell membranes.Several strategies are applied for nanocrystals production including precipitation,milling,high pressure homogenization and combination methods such as Nano-Edge^(TM),SmartCrystal and Precipitation-lyophilization-homogenization(PLH)technology.For oral administration,many publications reported useful advantages of nanocrystals to improve in vivo performances i.e.pharmacokinetics,pharmacodynamics,safety and targeted delivery which were discussed in this review.Additionally,transformation of nanocrystals to final formulations and future trends of nanocrystals were also described.
基金supported by the National Key Basic Research Special Foundation Project(2007CB106803)National Natural Science Foundation(40801111, 41001137)One hundred-Talent Plan of Chinese Academy of Sciences,the CAS/SAFEA International Partnership Program for Creative Research Teams,and the Program for Youthful Talents in Northwest A and F University
基金the Fondazione Cassa Risparmio di Firenze for kindly supporting this review study
文摘Andrographolide (AG) is the characteristic constituent of Andrographis paniculata, of the Acanthaceae family. This plant is a well-known Asian medicinal plant that is widely used in India, China, and Thailand. A monograph of Herba Andrographidis (Chuanxinlian) is included in the Chinese Pharmacopoeia, which reports that this decoction can “remove heat, counteract toxicity, and reduce swellings.” The numerous potential activities of AG range from anti-inflammatory to anti-diabetic action, from neuroprotection to antitumor activity, and from hepatoprotective to anti-obesity properties. However, AG has low bioavailability and poor water solubility, which can limit its distribution and accumulation in the body after administration. In addition, AG is not stable in gastrointestinal alkaline and acidic environments, and has been reported to have a very short half-life. Among the diverse strategies that have been adopted to increase AG water solubility and permeability, the technological approach is the most useful way to develop appropriate delivery systems. This review reports on published studies related to microparticles (MPs) and nanoparticles (NPs) loaded with AG. MPs based on polylactic-glycolic acid (PLGA), alginic acid, and glucan derivatives have been developed for parenteral oral and pulmonary administration, respectively. NPs include vesicles (both liposomes and niosomes);polymeric NPs (based on polyvinyl alcohol, polymerized phenylboronic acid, PLGA, human serum albumin, poly ethylcyanoacrylate, and polymeric micelles);solid lipid NPs;microemulsions and nanoemulsions;gold NPs;nanocrystals;and nanosuspensions. Improved bioavailability, target-tissue distribution, and efficacy of AG loaded in the described drug delivery systems have been reported.
基金financially supported by National Natural Science Foundation of China (No. 81502993)Doctoral Research Funding of Liaoning Province (No. 20141066)+1 种基金General Project in Department of Education of Liaoning Province (No. L2014379)Career Development Program for Young Teachers in Shenyang Pharmaceutical University
文摘The aim of this study was to improve the in vitro dissolution rate and oral bioavailability of oleanolic acid(OA), a water insoluble drug belonging to BCS class IV. Hot melt extrusion(HME) was applied to develop OA amorphous solid dispersions. The characterizations of the optimal formulation were performed by differential scanning calorimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy and in vitro dissolution test.The in vivo pharmacokinetic study was conducted in rats. As a result, OA solid dispersion based on PVP VA 64(OA-PVP) was successfully prepared. In the dissolution medium containing 0.3% SDS, OA-PVP dramatically increased the releasing rate of OA compared with the physical mixture(PM-PVP) and commercial tablet. Furthermore, OA-PVP exhibited higher AUC(P < 0.05) and Cmax(P < 0.05) than PM-PVP and commercial tablet. The superior dissolution property and bioavailability of OA-PVP mainly attributed to the amorphous state of OA in PVP VA64 and the well dispersion caused by thermal melting and shearing. Overall, hot melt extrusion was an efficient strategy to enhance the dissolution rate and oral bioavailability of OA.
基金The financial support from the National Key Research and Development Program of China (2017YFC1600306) is gratefully acknowledged。
文摘Background: The objective of this study was to determine the effects of supplementing Cu on growth performance, Cu metabolism and Cu-related enzyme activities of weanling pigs fed diets with two different Cu sources, and to estimate optimal Cu requirements and relative bioavailability from these two sources for pigs.Methods: Weanling pigs were allocated to 14 treatments arranged factorially, including 6 added Cu levels(5, 10,20, 40, 80, 160 mg/kg), and 2 mineral sources(tribasic Cu chloride, TBCC and copper proteinate, Cu Pro), as well as one negative control(0 mg/kg added Cu level) and one maximum allowed level treatment(200 mg/kg TBCC) for the entire 38-d experiment. Growth performance, mineral status and enzyme activities were measured at the end of this study.Results: Increasing levels of Cu showed linear and quadratic responses(P < 0.01) for final BW, ADG and FCR regardless of the sources. Supplementation with TBCC(> 80 mg/kg) and Cu Pro(> 20 mg/kg) significantly decreased(P < 0.05) diarrhea incidence of weanling pigs. There were linear and quadratic increases(P < 0.01) in bile, hepatic,and intestinal Cu concentrations, fecal Cu contents, and plasma enzyme activities(alkaline phosphatase,ceruloplasmin, Cu, Zn-Superoxide dismutase(Cu/Zn SOD), and glutathione peroxidase), whereas plasma malondialdehyde decreased(P < 0.01) linearly and quadratically as dietary Cu level increased. Similarly, pigs fed Cu Pro absorbed and retained more Cu and excreted less Cu than those fed TBCC when supplemented 80 mg/kg and above. Optimal dietary Cu requirements for pigs from 28 to 66 d of age estimated based on fitted broken-line models(P < 0.05) of bile Cu, plasma Cu/Zn SOD and growth performance were 93–140 mg/kg from TBCC, and 63–98 mg/kg from Cu Pro accordingly. According to slope ratios from multiple linear regression, the bioavailability value of Cu Pro relative to TBCC(100%) was 156–263%(P < 0.01).Conclusion: The findings indicated that Cu recommendation from current NRC(5–6 mg/kg) was not sufficient to meet the high requirement of weanling pigs. Cu from Cu Pro was significantly more bioavailable to weanling pigs than TBCC in stimulating growth and enzyme activities, decreasing diarrhea frequency and fecal Cu contents to the environment.
基金supported financially by the Subject Chief Scientist Program(10XD14303900)from Science and Technology Commission of Shanghai Municipalitythe Specialized Research Fund for the Doctoral Program of Higher Education of China(20123107110005).
文摘The objective of this study was to improve the dissolution and bioavailability of silymarin(SM).Solid dispersions(SDs)were prepared using solution-enhanced dispersion by supercritical fluids(SEDS)and evaluated in vitro and in vivo,compared with pure SM powder.The particle sizes,stability,and contents of residual solvent of the prepared SM-SDs with SEDS and solvent evaporation(SE)were investigated.Four polymer matrix materials were evaluated for the preparation of SM-SD-SEDS,and the hydrophilic polymer,polyvinyl pyrrolidone K17,was selected with a ratio of 1:5 between SM and the polymer.Physicochemical analyses using X-ray diffraction and differential scanning calorimetry indicated that SM was dispersed in SD in an amorphous state.The optimized SM-SD-SEDS showed no loss of SM after storage for 6 months and negligible residual solvent(ethanol)was detected using gas chromatography.In vitro drug release was increased from the SM-SDSEDS,as compared with pure SM powder or SM-SD-SE.In vivo,the area under the rat plasma SM concentration-time curve and the maximum plasma SM concentration were 2.4-fold and 1.9-fold higher,respectively,after oral administration of SM-SD-SEDS as compared with an aqueous SM suspension.These results illustrated the potential of using SEDS to prepare SM-SD,further improving the biopharmaceutical properties of this compound.
文摘Tea polyphenols(TPPs)have attracted significant research interest due to their health benefits.However,TPPs are sensitive to certain environmental and gastrointestinal conditions and their oral bioavailability was found to be very low.Delivery systems made of food-grade materials have been reported to improve the shelf-life,bioavailability and bioefficacy of TPPs.This review discusses the chemistry of TPPs;the setbacks of TPPs for application;and the strategies to counteract application limitations by rationally designing delivery systems.An overview of different formulations used to encapsulate TPPs is provided in this study,such as emulsion-based systems(liposome,nanoemulsion,double emulsion,and Pickering emulsion)and nano/microparticles-based systems(protein-based,carbohydrate-based,and bi-polymer based).In addition,the stability,bioavailability and bioactivities of encapsulated TPPs are evaluated by various in vitro and in vivo models.The current findings provide scientific insights in encapsulation approaches for the delivery of TPPs,which can be of great value to TPPs-fortified food products.Further explorations are needed for the encapsulated TPPs in terms of their applications in the real food industry as well as their biological fate and functional pathways in vivo.
文摘Although active constituents extracted from plants show robust in vitro pharmacological effects, low in vivo absorption greatly limits the widespread application of these compounds. A strategy of using phyto-phospholipid complexes represents a promising approach to increase the oral bioavailability of active constituents, which is consist of ‘‘label-friendly'phospholipids and active constituents. Hydrogen bond interactions between active constituents and phospholipids enable phospholipid complexes as an integral part. This review provides an update on four important issues related to phyto-phospholipid complexes: active constituents, phospholipids, solvents, and stoichiometric ratios. We also discuss recent progress in research on the preparation, characterization, structural verification, and increased bioavailability of phyto-phospholipid complexes.
基金Supported by AICTE-MODROBS Grant(Grant No.8024/RID/BOR/MOD458/2009-10)
文摘Recently,the use of herbal medicines has been increased all over the world due to their therapeutic effects and fewer adverse effects as compared to the modern medicines.However,many herbal drugs and herbal extracts despite of their impressive in-vitro findings demonstrates less or negligible in-vivo activity due to their poor lipid solubility or improper molecular size,resulting in poor absorption and hence poor bioavailability.Nowadays with the advancement in the technology,novel drug delivery systems open the door towards the development of enhancing bioavailability of herbal drug delivery systems.For last one decade many novel carriers such as liposomes,microspheres,nanoparticles,transferosomes,ethosomes,lipid based systems etc.have been reported for successful modified delivery of various herbal drugs.Many herbal compounds including quercetin,genistein,naringin,sinomenine,pipeline,glycvrrhizin and nitrile glycoside have demonstrated capability to enhance the bioavailability.The objective of this review is to summarize various available novel drug delivery technologies which have been developed for delivery of drugs(herbal),and to achieve better therapeutic response.An attempt has also been made to compile a profile on bioavailability enhancers of herbal origin with the mechanism of action(wherever reported)and studies on improvement in drug bioavailability,exhibited particularly by natural compounds.
文摘The effects of carbonate on the exchangeability and the bioavailability of exogenous neodymium in soil were studied by 147 Nd isotopic tracer method. Exchangeable Nd was extracted by 1 mol·L -1 NaAc (pH8 2) in the experiment. The results indicate that whether carbonate exists in soil or not, beyond 99% of exogenous Nd is adsorbed by soil. Low-concentration carbonate (0 8～1 6 g·kg -1 ) can reduce exchangeable Nd concentration in soil, while high-concentration carbonate (4 0 g·kg -1 ) impacts little on the exchangeable Nd concentration. In addition, carbonate of 0 8～1 6 g·kg -1 in soil can inhibit wheat seedlings to absorb Nd. However, when the carbonate concentration rises to 4 0 g·kg -1 , the inhibition will become indistinct.
文摘Two hundred and sixty four broiler breeder hens of 32 weeks of age were distributed randomly in four dietary treatments. The dietary treatments were T0: Broiler breeder ration containing 40 ppm zinc (basal 29.8 ppm + 10.2 ppm inorganic zinc), T1: T0 + organic zinc (zinc methionine) @ 20 ppm, T2: T0 + organic zinc @ 40 ppm and T3: T0 + organic zinc @ 60 ppm. The experiment was continued from 32 to 48 weeks of age. At 48 weeks, the weight of lymphoid organs, zinc levels in organs and immunity response were determined. The faecal zinc level was determined at monthly interval. The weight lymphoid organs of different treatment groups (both organic and inorganic zinc fed groups) of the broiler breeders did not differ significantly (P > 0.05). The cellular immune response of breeder birds to PHA-P was significantly (P 0.05) higher in group T3 than the rest of treated groups. The antibody titre to SRBC differed among the treated groups. The zinc content of serum of broiler breeders of all the groups did not differ significantly (P > 0.05) in all the periods of study. Zinc content in liver and tibia of broiler breeders in different dietary treatments of zinc differed significantly (P 0.05) with higher levels were obtained on increasing zinc concentration in the diet. The zinc level in the spleen and kidney of the broiler breeders in different dietary treatments did not differ significantly (P > 0.05). The average zinc content in the faeces of broiler breeder during 35 to 43 week of age did not differ significantly (P > 0.05) among the treated groups. At 48 weeks of age, zinc content of the faeces of T3 was found to be significantly (P 0.05) higher than the rest of treated groups. Similarly, during the overall experimental period analysis, it was found that zinc levels in the faeces of T2 and T3 were significantly (P 0.05) higher than T1 and T0.
基金special construction projects fund which belongs to“Taishan Scholar-Pharmacy Specially Recruited Experts”.
文摘Numerous systems have been designed during the past three decades to improve bioavailability of ophthalmic drug delivery,including:ocular prodrugs and nanotechnology-based drug delivery system.The former can improve the efficacy of ocular drug via enhancing corneal penetration of ocular drugs,prolonging their duration of action and/or reducing the systemic side-effects,unfortunately,some characteristics of the pro-drugs,such as poorly aqueous stability,poorly aqueous solubility and severe eye irritation probably,limit their clinical practice and cannot be ignored.As we all know,nanotech-nology for ocular drug delivery can carry poorly soluble drugs,protect the encapsulated molecules from hydrolysis,control the rate of drug delivery and prolong the precorneal retention of drugs.All of these merits may solve the problems in the utilization of ocular prodrugs and increase the bioavailability of ocular drug delivery.By reviewing recent ad-vances of prodrugs and nanostructures in ocular drug delivery,this paper focus specifically on the promising prospects of nanocarriers overcoming the drawbacks of prodrugs for ophthalmic drug delivery by precorneal routes.
文摘The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomized 2 way crossover study. The concentrations in plasma were determined by HPLC UV method. The main parameters of irbesartan capsules were: C max : 1.502±0.295 μg/ml, t max : 1.44±0.34 h, t 1/2 : 20.21±14.71 h, AUC 0 t : 11.087±3.443 μg/ml -1 ·h. The relative bioavailability of capsule to tablet was (101.4±28.9) %. The results of statistical analysis showed that two formulations were bioequivalent.
文摘Objectives: Vitamin E is an important human lipophilic antioxidant and is required for many metabolic functions. A high vitamin E intake appears to favorably impact a variety of disease processes. The vitamin E intake, excluding sup-plemental intake, of the vast majority of adults is below the current recommended level. By consuming vitamin E-enriched food, it is possible to take in adequate amounts of vitamin E. Vitamin E intake from enriched foods might prevent certain diseases without the need to ingest specific vitamin E supplements. The vitamin E that is present in enriched foods has to exhibit maximal bioavailability to ensure a sufficient intake of vitamin E from one portion of fortified food. The aim of the present study was to develop an enriched food that has highly bioavailable vitamin E. Furthermore, we wanted to examine whether vitamin E bioavailability can be affected by the technological properties of fortified food. Methods: Volunteers were given test foods (cream cheese and mayonnaise) that had been fortified with 60 mg of RRR-α-tocopherol. The test foods were technologically modified and the bioavailability of RRR-α-tocopherol was determined via a short-term kinetic measurement, which was 24 h long, and a long-term kinetic measurement, which was 28 d long. The test foods were characterized with respect to matrix properties. Results: In comparison to the mayonnaise group the serum α-tocopherol area under the curve (AUC) was significantly higher in the cream cheese group, as shown in the short-term kinetic (p = 0.010) and long-term kinetic (p = 0.017) studies. Conclusions: In conclusion, RRR-α-tocopherol was more bioavailable in cream cheese than in mayonnaise in both short-term and long-term periods. Hence, food matrices affect bioavailability of RRR-α-tocopherol. Fortified foods with proven high α-tocopherol bioavailabilities could be merchandised as functional foods with diseases prevention properties.
文摘Objective:To enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract by formulating its nanosuspension.Methods:Nanoprecipitation approach was used for the formulation of nanosuspension using polysorbate-80 as a stabilizer.The formulated nanosuspension was assessed for particle size,polydispersity index,zeta potential value and for in vitro dissolution study.Oral bioavailability studies were carried out in Wistar male albino rats by administering a single dose(50 mg/kg.b.wt)of the formulated nanosuspension and coarse suspension.The storage stability of the formulated nanosuspension was determined after three months of storage at room temperature and under the refrigerated condition.Mutagenicity assay was carried out to evaluate the toxicity of the formulated nanosuspension using two mutant strains(Salmonella typhimurium TA100 and Salmonella typhimurium TA98).Results:The mean particle size of the formulated nanosuspension was 90.53 nm with polydispersity index and zeta potential values of 0.175 and-15.7 m V,respectively.Terminalia arjuna nanosuspension showed improved dissolution rate and 1.33-fold higher oral bioavailability than its coarse suspension.The formulated nanosuspension also showed better stability under the refrigerated condition and was non-mutagenic against both strains.Conclusions:Our study demonstrates that nanosuspension technology can effectively enhance the dissolution rate and oral bioavailability of Terminalia arjuna bark extract.
文摘The in vivo bioavailability of soy protein isolates and corn zein film material before and after film formation by heat/ pressure was determined. The In vitro digestibility of corn zein before and after film formation was also measured. Films were produced from anhydrous protein with 30% glycerol added using a heat-press method with no use of casting solvents or cross-linking agents. Corn zein raw and film material were ground under liquid nitrogen then digested in two enzyme-acid cocktails with free amino acid analysis before and after digestion. The protein efficiency ratio and net protein ratio were determined for both zein and soy protein using a weanling Sprague-Dawley descended rat feeding study. The In vitro digestibility study indicated that the non-heat pressed corn zein was more digestible than the heat pressed zein. However, the in vivo results indicated that corn and soy protein were equally bioavailable whether they were derived from film mixture prior to or after film formation. Both corn zein and soy protein material had lower protein efficiency ratio than the control diet. Furthermore, soy protein films materials had a higher protein efficiency ratio than corn zein.
