Traditional drug delivery methods are prone to large fluctuations in drug concentration and require multiple frequent doses.As a green material with excellent properties,cellulose has been widely used as a drug carrie...Traditional drug delivery methods are prone to large fluctuations in drug concentration and require multiple frequent doses.As a green material with excellent properties,cellulose has been widely used as a drug carrier for the development and preparation of drug controlled-release system.Based on the mechanisms of slow drug release,such as dissolution-diffusion release,degradation release,and nanochannel-controlled release,the preparation methods of cellulose-based drug carriers are introduced in this paper.The applications of cellulose-based drug carriers in the fields of antitumor therapy,antibacterial therapy,chronic disease treatment,and viral disease treatment are summarized with the aim of providing a useful reference for research on cellulose-based drug carriers.展开更多
Potential of nanoscale triazine based dendritic macromolecules G1,G2 and G3 as solubility enhancers of drug was investigated.Effect of pH,concentration and generation of synthesized dendritic macromolecules on solubil...Potential of nanoscale triazine based dendritic macromolecules G1,G2 and G3 as solubility enhancers of drug was investigated.Effect of pH,concentration and generation of synthesized dendritic macromolecules on solubility of ketoprofen was studied.G3 dendrimer was further exploited as carrier for sustained release.Ketoprofen was encapsulated by inclusion complex method and also characterized by Flourier Transform Infrared spectroscopy.Sustained release study of ketoprofen from ketoprofen loaded dendrimer was carried out and compared with free ketoprofen.Hemolytic potential and Cytotoxicity assay using A-549 lung cancer cell lines revealed that synthesized triazine based dendritic macromolecules having more potential that commercially available PAMAM dendrimer.展开更多
Bone tumour is one of most common primary cancer which exhibits cancerous osteoblastic differentiation and malignant osteoid in patients.At present,chemotherapy(pre-and post-operative)is used as a standard treatment p...Bone tumour is one of most common primary cancer which exhibits cancerous osteoblastic differentiation and malignant osteoid in patients.At present,chemotherapy(pre-and post-operative)is used as a standard treatment protocol for bone tumour.However,drugs used in the treatment of bone tumour induce high toxicity to normal tissues including anaemia,neutropenia,thrombocytopenia,and heart damage which further reduce the survival rate of patients.Therefore,there is an urgent need to develop a new therapeutic approach for the treatment such that it induce maximum cell killing effect in tumor cells while sparing the healthy bone cells.In this article,some new perspectives were provided on the development of bone-targeted nano-drug carriers for bone cancer treatment.We hope such discussions wouldencourage more detailed and careful studies to support product development of bone-targeted drug carriers for bone cancer treatment.展开更多
The objective of this review is to outline the application of bicelles(or called bilayer micelles)and bilayer nanodisks in pharmaceutics,pharmaceutical analysis and biochemistry.The application of open disk-like struc...The objective of this review is to outline the application of bicelles(or called bilayer micelles)and bilayer nanodisks in pharmaceutics,pharmaceutical analysis and biochemistry.The application of open disk-like structures as model membrane and drug carrier has been described.The exploration of many reports in different fields suggested that these open disk-like structures have great potential in studying interactions between drug-membrane and structure/function studies of membrane-bound proteins.Furthermore,they could be applied as promising carriers for in vivo delivery of drugs,protein and peptide.展开更多
Berberine(BBR)is an isoquinoline alkaloid that can be extracted from the traditional Chinese medicine Huang Lian.It has anti-inflammatory,anti-cancer,protection of nerves,hypoglycemic,blood lipid,anti-oxidation,antiba...Berberine(BBR)is an isoquinoline alkaloid that can be extracted from the traditional Chinese medicine Huang Lian.It has anti-inflammatory,anti-cancer,protection of nerves,hypoglycemic,blood lipid,anti-oxidation,antibacterial and other effects.It can be used clinically to treat chronic colitis,bacterial vaginitis,rheumatoid arthritis,breast cancer,liver cancer,Alzheimer's disease,diabetes,obesity and other common diseases.This paper reviews the pharmacological effects of berberine and the research progress of effective drug carriers in order to provide new ideas for the clinical application of berberine.展开更多
Fe_3O_4/carbon nanotubes(Fe_3O_4/CNTs) nanocomposites were prepared by polylol hightemperature decomposition of the precursor ferric chloride and CNTs in liquid triethylene glycol.After surface modification with hexan...Fe_3O_4/carbon nanotubes(Fe_3O_4/CNTs) nanocomposites were prepared by polylol hightemperature decomposition of the precursor ferric chloride and CNTs in liquid triethylene glycol.After surface modification with hexanediamine,folate was covalently linked to the amine group of magnetic Fe_3O_4/CNTs nanocomposites.The products were characterized by Fourier-transform infrared spectroscopy,transmission electron microscopy,and vibrating sample magnetometry.Then Fe_3O_4/CNTs were used as a dual-drug carrier to co-delivery of the hydrophilic drug epirubicin hydrochloride and hydrophobic drug paclitaxel.The results indicated that the Fe_3O_4/CNTs had a favorable release property for epirubicin and paclitaxel,and thus had potential application in tumor-targeted combination chemotherapy.展开更多
Molecular imprinted nanoparticles(MINPs) can memorize the shape and functional group positions complementary to template, which account for the large drug loading capacity and slow drug release behavior as drug carrie...Molecular imprinted nanoparticles(MINPs) can memorize the shape and functional group positions complementary to template, which account for the large drug loading capacity and slow drug release behavior as drug carriers. We synthesized MINPs via precipitation polymerization with vinblastine(VBL) as a model drug, and investigated the drug loading,releasing property in vitro and bio-distribution in vivo. The obtained MINPs, from 300 to 450 nm,had smooth surface and favorable dispersibility. The entrapment efficacy and drug loading capacity of VBL loaded MINPs(MINPs-VBL) were 83.25% and 8.72% respectively. In PBS(pH 7.4),MINPs-VBL showed sustained release behavior. The cumulative release percentage reached about 70% during 216 h and no burst release was observed. The releasing behavior of MINPsVBL in vitro conformed to the first-order kinetics model. MINPs-VBL and commercially available vinblastine sulfate injection(VBL injection) were injected via tail vein of SD rats respectively to investigate the bio-distribution. MINPs-VBL group showed higher concentration of VBL in tissues and serum than VBL injection group after 60 min, and the drug level in liver was the highest. MINPs-VBL exhibited liver targeting trend to some extent, which was based on the evaluation of drug targeting index(DTI) and drug selecting index(DSI).展开更多
β-TCP ceramics drug carrier was first prepared and characterized. SEM showed that β-TCP carrier was in porous amorphous structure with diameters around 10 μm. The physical properties including apparent porosity, vo...β-TCP ceramics drug carrier was first prepared and characterized. SEM showed that β-TCP carrier was in porous amorphous structure with diameters around 10 μm. The physical properties including apparent porosity, volume-weight, tensile strength and the permeability were measured and the results indicated those properties fit the clinical usage of β-TCP drug carrier. Furthermore, drug release experiment in vitro showed that the carrier could prolong drug release in simulated body fluid which provides basis for the clinical use of β-TCP ceramics as drug carrier.展开更多
Diblock copolymer poly(ethylene glycol) methyl ether–polylactide (MePEG–PLA) micelles were prepared by dialysis against water. Indomethacin (IMC) as a model drug was entrapped into the micelles by dialysis method. T...Diblock copolymer poly(ethylene glycol) methyl ether–polylactide (MePEG–PLA) micelles were prepared by dialysis against water. Indomethacin (IMC) as a model drug was entrapped into the micelles by dialysis method. The critical micelle concentration (CMC) of the prepared micelles in distilled water investigated by fluorescence spectroscopy was 0.0051 mg/mL which is lower than that of common low molecular weight surfactants. The diameters of MePEGPLA micelles and IMC loaded MePEGPLA micelles in a number-averaged scale measured by dynamic light scattering were 52.4 and 53.7 nm respectively. The observation with transmission electron microscope and scanning electron microscope showed that the appearance of MePEGPLA micelles was in a spherical shape. The content of IMC incorporated in the core portion of the micelles was 18% (ω). The effects of the synthesis method of the copolymer on the polydispersity of the micelles and the yield of the micelles formation were discussed.展开更多
Methoxy poly(ethylene glycol)-poly(D,L-lactide) block copolymers (PEG-PLA) were prepared through ring-opening polymerization.The oil in water suspension method was used to prepare block copolymer micelles. The critica...Methoxy poly(ethylene glycol)-poly(D,L-lactide) block copolymers (PEG-PLA) were prepared through ring-opening polymerization.The oil in water suspension method was used to prepare block copolymer micelles. The critical micelle concentration (CMC) by fluorescence spectroscopy was 0.0056 mg·ml -1 . The physical state of the inner core region of micelles was characterized with 1HNMR. The size of indomethacin (IMC) loaded micelles measured by dynamic light scattering (DLS) showed narrow monodisperse size distribution and the average diameters were less than 50 nm. In addition, the nanoparticles with relatively high drug loading content (DLC) were obtained.展开更多
Drug carrier biocompatible and biodegradable nanoparticles of about 15 nm were prepared by solvent evaporation technique from star-shaped poly(D,L-lactide) synthesized using dipentaerythritol as core and Tin (II) ethy...Drug carrier biocompatible and biodegradable nanoparticles of about 15 nm were prepared by solvent evaporation technique from star-shaped poly(D,L-lactide) synthesized using dipentaerythritol as core and Tin (II) ethylhexanoate as catalyst.展开更多
Long-circulating drug carriers are highly desirable in drug delivery system.However,nonspecific protein adsorption leaves a great challenge in drug delivery of intravenous administration and significantly affects both...Long-circulating drug carriers are highly desirable in drug delivery system.However,nonspecific protein adsorption leaves a great challenge in drug delivery of intravenous administration and significantly affects both the pharmacokinetic profiles of the carrier and drugs,resulting in negatively affect of therapeutic efficiency.Therefore,it is important to make surface modification of drug carriers by protein-resistant materials to prolong the blood circulation time and increase the targeted accumulation of therapeutic agents.In this review,we highlight the possible mechanism of protein resistance and recent progress of the alternative protein-resistant materials and their drug carriers,such as poly(ethylene glycol),oligo(ethylene glycol),zwitterionic materials,and red blood cells adhesion.展开更多
The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation time.For most drugs,sufficient in vivo circulation time is the basis of high bioavail...The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation time.For most drugs,sufficient in vivo circulation time is the basis of high bioavailability.Drug carrier plays an irreplaceable role in helping drug avoid being quickly recognized and cleared by mononuclear phagocyte system,to give drug enough time to arrive at targeted organ and tissue to play its therapeutic effect.The physical and chemical properties of drug carriers,such as size,shape,surface charge and surface modification,would affect their in vivo circulation time,metabolic behavior and biodistribution.The final circulation time of carriers is determined by the balance between macrophage recognitions,blood vessel penetration and urine excretion.Therefore,when designing the drug delivery system,we should pay much attention to the properties of drug carriers to get enough in vivo circulation time to arrive at target site eventually.This article mainly reviews the effect of carrier size,size,surface charge and surface properties on its circulation time in vivo,and discusses the mechanism of these properties affecting circulation time.This review has reference significance for the research of long-circulation drug delivery system.展开更多
This paper reports on the synthesis and characterization of 4 nm magnetite nanoparticles coated with amphiphilic block copolymers of poly(ethyl methacrylate)-b-poly(2-hydroxyethyl methacrylate) (PEMA- b-PHEMA) by surf...This paper reports on the synthesis and characterization of 4 nm magnetite nanoparticles coated with amphiphilic block copolymers of poly(ethyl methacrylate)-b-poly(2-hydroxyethyl methacrylate) (PEMA- b-PHEMA) by surface-initiated atom transfer radical polymerization (ATRP), which can act as new potential carriers for hydrophobic targeted drug delivery. Vibrating sample magnetometer analysis indi-cated that the magnetite nanoparticles were superparamagnetic at room temperature. Thermogravim-etric analysis (TGA) was applied to studying the property of surface of magnetite nanoparticles, and the surface density of macromolecules was calculated. The grafting density of oleic acid, BrMPA and PEMA was 5.8, 3.9, 0.16 chain/nm2 respectively, which indicates that the initiation efficiency decreases due to the influence of large space of oleic acid molecules. In vitro progesterone and (-)-isoproterenol hy-drochloride release in phosphate buffered saline (PBS) at pH 7.0 and 37℃ was conducted in order to demonstrate the function of drug loading and release. The results showed that the amount of drug carried into the core-shell Fe3O4@PEMA-b-PHEMA depends on the length of hydrophobic segment of block copolymer. The release of progesterone (37% after 22 h in our previous work) was compared with the release of (-)-isoproterenol hydrochloride (80% after 50 min), demonstrating that the strong hy-drophobic interaction between hydrophobic segment and drug can effectively control the release of hydrophobic drugs.展开更多
Dialdehyde starch nanoparticles (DASNP) were prepared by the redox reaction of NaIO4 and starch in water-in-oil microemulsion. IR spectrum showed that DASNP had aldehyde groups, and quantitative alkali consumption sho...Dialdehyde starch nanoparticles (DASNP) were prepared by the redox reaction of NaIO4 and starch in water-in-oil microemulsion. IR spectrum showed that DASNP had aldehyde groups, and quantitative alkali consumption showed that its dialdehyde content was about (50±5)%. The average diameter of DASNP determined by SEM was about 100 nm. TGA-DTA showed that its thermal stability was better than starch nanoparticle (StNP) and dialdehyde starch (DAS). Its low biological toxicity was detected by cell experiment. Also the best mass ratio of doxorubicin (DOX) to combined DASNP detected by UV-VIS was 15 : 1, and the product was effective for controlled release of DOX. The cell experiment showed that the drug-carrier particle (DOX-DASNP) can release DOX for a long time and strengthened the effect of the anticancer drug. This work demonstrates that the DASNP, which has good thermal stability, small particle size, low biological toxicity, and slowly anticancer drug-releasing to strengthen drug effect, is a potentially useful carrier for anticancer drug.展开更多
To design a new type of antitumor nanodrug carrier with good biocompatibility, a drug delivery system with a 2.19% drug-loading rate, measured by high-performance liquid chromatography(HPLC), was prepared by membrane ...To design a new type of antitumor nanodrug carrier with good biocompatibility, a drug delivery system with a 2.19% drug-loading rate, measured by high-performance liquid chromatography(HPLC), was prepared by membrane hydration using a mixed polymer: Pluronic■ F-127, which binds folic acid(FA), Pluronic■ F-68 and triptolide(TPL)(FA-F-127/F-68-TPL). As a control, another drug delivery system based on a single polymer(FA-F-127-TPL) with a 1.90% drug-loading rate was prepared by substituting F-68 with F-127. The average particle sizes of FA-F-127/F-68-TPL and FA-F-127-TPL measured by a particle size analyzer were 30.7 nm and 31.6 nm, respectively. Their morphology was observed by atomic force microscopy(AFM). The results showed that FA-F-127-TPL self-assembled into nanomicelles, whereas FA-F-127/F-68-TPL self-assembled into nanogels. An MTT assay showed that a very low concentration of FA-F-127/F-68-TPL or FA-F-127-TPL could significantly inhibit the proliferation of multidrug-resistant(MDR) breast cancer cells(MCF-7/ADR cells) and induce cell death. The effects were significantly different from those of free TPL(P < 0.01). Using the fluorescent probe Nile red(Nr) as the drug model, FA-F-127/F-68-Nr nanogels and FAF-127-Nr nanomicelles were prepared and then incubated with human hepatocarcinoma(HepG2) and MCF-7/ADR cells, and the fluorescence intensity in the cells was measured by a multifunctional microplate reader. The results indicated that both FA-F-127/F-68-Nr and FA-F-127-Nr had sustained release in the cells, but HepG2 and MCF-7/ADR cells exhibited significantly higher endocytosis of FA-F-127/F-68-Nr than that of FA-F-127-Nr(P < 0.01). A nude mice transplanted tumor model was prepared to monitor FA-F-127/F-68-Nr in the tumor tissue and organs by whole-body fluorescent imaging. The results showed that FA-F-127/F-68-Nr targeted tumor tissues. The prepared nanogels had small particle size, were easy to swallow, exhibited slow release property,targeted tumor cells, and could improve the antitumor effects of TPL;hence, they are ideal carriers for low-dose antineoplastic drugs.展开更多
One-pot synthesis of magnetic nanogels with excellent biocompatibility via the photochemical method is reported in this paper.Poly(PEGMA) modified superparamagnetic nanogels(poly(PEGMA) magnetic nanogels) were synthes...One-pot synthesis of magnetic nanogels with excellent biocompatibility via the photochemical method is reported in this paper.Poly(PEGMA) modified superparamagnetic nanogels(poly(PEGMA) magnetic nanogels) were synthesized by in-situ polymerization using poly(ethylene glycol) methacrylate(PEGMA) as the monomer and N,N'-methylene-bis-(acrylamide)(MBA) as the cross-linking agent in magnetite aqueous suspension under UV irradiation.The surface functional groups and components of magnetic nanogels were analyzed by Fourier transform infrared spectroscopy(FTIR) and a thermogra-vimetric analyzer(TGA).The results indicated that the poly(PEGMA) magnetic nanogels were synthe-sized successfully by coating poly(PEGMA) on the Fe3O4 nanoparticles under UV irradiation,and the Fe3O4 nanoparticles content in this nanogels was above 50 wt%.The morphology,size,zeta-potential and magnetic property were also characterized.The magnetic nanogels had a nearly spherical shape and core-shell structure,the average size in aqueous system measured by photon correlation spec-troscopy(PCS) was 68.4 nm,which was much bigger than that in the dry state,the nanogels behaved superparamagnetically with saturated magnetization of 58.6 emu/g,and the zeta-potential was-16.3-_17.3 mV at physiological pH(6.8-7.4) which could help to maintain stability in blood.The preliminary application as drug carrier was made and the doxorubicin-loaded magnetic nanogels had an excellent property in slow-release.The experiment indicated that the magnetic nanogel was an ideal candidate carrier in target drug delivery systems and other biomedical application.展开更多
Amphiphilic diblock copolymers composed of methoxy polyethylene glycol (MePEG) and poly(D,L- lactide) (PDLLA) were prepared for the preparation of polymeric micelles. The use of MePEG-PDLLA as drug carriers has been r...Amphiphilic diblock copolymers composed of methoxy polyethylene glycol (MePEG) and poly(D,L- lactide) (PDLLA) were prepared for the preparation of polymeric micelles. The use of MePEG-PDLLA as drug carriers has been reported in the open literature, but there are only few data on the application of a se- ries of MePEG-PDLLA copolymers with different lengths in the medical field. The shape of the polymeric mi- celles is also important in drug delivery. Studies on in vitro drug release profiles require a good sink condi- tion. The critical micelle concentration of a series of MePEG-PDLLA has a significant role in drug release. To estimate their feasibility as a drug carrier, polymeric micelles made of MePEG-PDLLA block copolymer were prepared by the oil in water (O/W) emulsion method. From dynamic light scattering (DLS) measurements, the size of the micelle formed was less than 200 nm. The critical micelle concentration of polymeric micelles with various compositions was determined using pyrene as a fluorescence probe. The critical micelle con- centration decreased with increasing number of hydrophobic segments. MePEG-PDLLA micelles have a considerably low critical micelle concentration (0.4-0.5 μg/mL), which is apparently an advantage in utilizing these micelles as drug carriers. The morphology of the polymeric micelles was observed using scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The micelles were found to be nearly spherical. The yield of the polymeric micelles obtained from the O/W method is as high as 85%.展开更多
Nano-carbon and iron composite―carbon-coated iron nanoparticles (CCINs) produced by carbon arc method can be used as a new kind of magnetic targeting induction heating drug carrier for cancer therapy. The structure a...Nano-carbon and iron composite―carbon-coated iron nanoparticles (CCINs) produced by carbon arc method can be used as a new kind of magnetic targeting induction heating drug carrier for cancer therapy. The structure and morphology of CCINs are studied by X-ray diffraction (XRD) and transmission electron microscope (TEM). Mossbauer spectra of these nanoparticles show that they contain only iron and carbon, without ferric carbide and ferric oxide. CCINs can be used as the magnetic drug carrier, with the effect of targeting magnetic induction heating in its inner core and higher drug adsorption in its nano-carbon shell outside because of its high specific surface area. CCINs can absorb Epirubicin (EPI) of 160 μg/mg measured by an optical spectrometer. In acute toxicity experiment with mice, the median lethal dose (LD50) of EPI is 16.9 mg/kg, while that of EPI-CCINs mixture is 20.7 mg/kg and none of the mice died after pure CCINs medication. The results show that pure CCINs belong to non-toxic grade and EPI delivery in mixture with CCINs can reduce its acute toxicity in mice. The magnetic properties of CCINs and their magnetic induction heating are investigated. The iron nanoparticle in its inner core has better magnetism with a good effect on targeting magnetic induction heating. When the CCINs are mixed with physiological salt water and are injected uniformly in pig's liver, the temperature goes up to 48℃. While in the case that CCINs are filled in a certain section of pig's liver, the temperature goes up to 52℃. In both cases the temperature is high enough to kill the cancer cell. CCINs have potential applications in cancer therapy.展开更多
基金Shaanxi Province College Student Innovation and Entrepreneurship Training Program Project(Project Number:S202310708098).
文摘Traditional drug delivery methods are prone to large fluctuations in drug concentration and require multiple frequent doses.As a green material with excellent properties,cellulose has been widely used as a drug carrier for the development and preparation of drug controlled-release system.Based on the mechanisms of slow drug release,such as dissolution-diffusion release,degradation release,and nanochannel-controlled release,the preparation methods of cellulose-based drug carriers are introduced in this paper.The applications of cellulose-based drug carriers in the fields of antitumor therapy,antibacterial therapy,chronic disease treatment,and viral disease treatment are summarized with the aim of providing a useful reference for research on cellulose-based drug carriers.
文摘Potential of nanoscale triazine based dendritic macromolecules G1,G2 and G3 as solubility enhancers of drug was investigated.Effect of pH,concentration and generation of synthesized dendritic macromolecules on solubility of ketoprofen was studied.G3 dendrimer was further exploited as carrier for sustained release.Ketoprofen was encapsulated by inclusion complex method and also characterized by Flourier Transform Infrared spectroscopy.Sustained release study of ketoprofen from ketoprofen loaded dendrimer was carried out and compared with free ketoprofen.Hemolytic potential and Cytotoxicity assay using A-549 lung cancer cell lines revealed that synthesized triazine based dendritic macromolecules having more potential that commercially available PAMAM dendrimer.
基金The project supported by National Natural Science Foundation of China(81300964)the China Postdoctoral Science Foundation(2013M531611,2014T70648)
文摘Bone tumour is one of most common primary cancer which exhibits cancerous osteoblastic differentiation and malignant osteoid in patients.At present,chemotherapy(pre-and post-operative)is used as a standard treatment protocol for bone tumour.However,drugs used in the treatment of bone tumour induce high toxicity to normal tissues including anaemia,neutropenia,thrombocytopenia,and heart damage which further reduce the survival rate of patients.Therefore,there is an urgent need to develop a new therapeutic approach for the treatment such that it induce maximum cell killing effect in tumor cells while sparing the healthy bone cells.In this article,some new perspectives were provided on the development of bone-targeted nano-drug carriers for bone cancer treatment.We hope such discussions wouldencourage more detailed and careful studies to support product development of bone-targeted drug carriers for bone cancer treatment.
文摘The objective of this review is to outline the application of bicelles(or called bilayer micelles)and bilayer nanodisks in pharmaceutics,pharmaceutical analysis and biochemistry.The application of open disk-like structures as model membrane and drug carrier has been described.The exploration of many reports in different fields suggested that these open disk-like structures have great potential in studying interactions between drug-membrane and structure/function studies of membrane-bound proteins.Furthermore,they could be applied as promising carriers for in vivo delivery of drugs,protein and peptide.
基金Jilin Science and Technology Development Project(No.20190303183SF)Undergraduate Teaching Reform research Project of Jilin University(No.2019XYB318)
文摘Berberine(BBR)is an isoquinoline alkaloid that can be extracted from the traditional Chinese medicine Huang Lian.It has anti-inflammatory,anti-cancer,protection of nerves,hypoglycemic,blood lipid,anti-oxidation,antibacterial and other effects.It can be used clinically to treat chronic colitis,bacterial vaginitis,rheumatoid arthritis,breast cancer,liver cancer,Alzheimer's disease,diabetes,obesity and other common diseases.This paper reviews the pharmacological effects of berberine and the research progress of effective drug carriers in order to provide new ideas for the clinical application of berberine.
基金Funded by Natural Science Fund of Jiangsu Overseas Research&Training Program for University Prominent Young&Middleaged Teachers and Presidents,the Natural Science Fund of Jiangsu Province(No.BK20130094)the Enterprise-universities Cooperative Innovation Fund of Jiangsu Province(No.BY2014016)
文摘Fe_3O_4/carbon nanotubes(Fe_3O_4/CNTs) nanocomposites were prepared by polylol hightemperature decomposition of the precursor ferric chloride and CNTs in liquid triethylene glycol.After surface modification with hexanediamine,folate was covalently linked to the amine group of magnetic Fe_3O_4/CNTs nanocomposites.The products were characterized by Fourier-transform infrared spectroscopy,transmission electron microscopy,and vibrating sample magnetometry.Then Fe_3O_4/CNTs were used as a dual-drug carrier to co-delivery of the hydrophilic drug epirubicin hydrochloride and hydrophobic drug paclitaxel.The results indicated that the Fe_3O_4/CNTs had a favorable release property for epirubicin and paclitaxel,and thus had potential application in tumor-targeted combination chemotherapy.
基金supported by the National Natural Science Foundation of China (grant number: 81173566)
文摘Molecular imprinted nanoparticles(MINPs) can memorize the shape and functional group positions complementary to template, which account for the large drug loading capacity and slow drug release behavior as drug carriers. We synthesized MINPs via precipitation polymerization with vinblastine(VBL) as a model drug, and investigated the drug loading,releasing property in vitro and bio-distribution in vivo. The obtained MINPs, from 300 to 450 nm,had smooth surface and favorable dispersibility. The entrapment efficacy and drug loading capacity of VBL loaded MINPs(MINPs-VBL) were 83.25% and 8.72% respectively. In PBS(pH 7.4),MINPs-VBL showed sustained release behavior. The cumulative release percentage reached about 70% during 216 h and no burst release was observed. The releasing behavior of MINPsVBL in vitro conformed to the first-order kinetics model. MINPs-VBL and commercially available vinblastine sulfate injection(VBL injection) were injected via tail vein of SD rats respectively to investigate the bio-distribution. MINPs-VBL group showed higher concentration of VBL in tissues and serum than VBL injection group after 60 min, and the drug level in liver was the highest. MINPs-VBL exhibited liver targeting trend to some extent, which was based on the evaluation of drug targeting index(DTI) and drug selecting index(DSI).
基金Funded by the "973" Chinese National Key Fundamental Research and Development Program (No.G1999064701)the Research Fund of Key Laboratory for Advanced Technology in Environmental Protection of Jiangsu Province (AE201037)
文摘β-TCP ceramics drug carrier was first prepared and characterized. SEM showed that β-TCP carrier was in porous amorphous structure with diameters around 10 μm. The physical properties including apparent porosity, volume-weight, tensile strength and the permeability were measured and the results indicated those properties fit the clinical usage of β-TCP drug carrier. Furthermore, drug release experiment in vitro showed that the carrier could prolong drug release in simulated body fluid which provides basis for the clinical use of β-TCP ceramics as drug carrier.
基金National Natural Science Foundation of China (No.29836130)
文摘Diblock copolymer poly(ethylene glycol) methyl ether–polylactide (MePEG–PLA) micelles were prepared by dialysis against water. Indomethacin (IMC) as a model drug was entrapped into the micelles by dialysis method. The critical micelle concentration (CMC) of the prepared micelles in distilled water investigated by fluorescence spectroscopy was 0.0051 mg/mL which is lower than that of common low molecular weight surfactants. The diameters of MePEGPLA micelles and IMC loaded MePEGPLA micelles in a number-averaged scale measured by dynamic light scattering were 52.4 and 53.7 nm respectively. The observation with transmission electron microscope and scanning electron microscope showed that the appearance of MePEGPLA micelles was in a spherical shape. The content of IMC incorporated in the core portion of the micelles was 18% (ω). The effects of the synthesis method of the copolymer on the polydispersity of the micelles and the yield of the micelles formation were discussed.
文摘Methoxy poly(ethylene glycol)-poly(D,L-lactide) block copolymers (PEG-PLA) were prepared through ring-opening polymerization.The oil in water suspension method was used to prepare block copolymer micelles. The critical micelle concentration (CMC) by fluorescence spectroscopy was 0.0056 mg·ml -1 . The physical state of the inner core region of micelles was characterized with 1HNMR. The size of indomethacin (IMC) loaded micelles measured by dynamic light scattering (DLS) showed narrow monodisperse size distribution and the average diameters were less than 50 nm. In addition, the nanoparticles with relatively high drug loading content (DLC) were obtained.
文摘Drug carrier biocompatible and biodegradable nanoparticles of about 15 nm were prepared by solvent evaporation technique from star-shaped poly(D,L-lactide) synthesized using dipentaerythritol as core and Tin (II) ethylhexanoate as catalyst.
基金This work was supported by the National Natural Science Foundation of China(21304099,51203162,51103159,51373177)the National High Technology Research and Development Program(2014AA020708,2012AA022703,2012AA020804)+3 种基金the Instrument Developing Project of the Chinese Academy of Sciences(YZ201253,YZ201313)the Open Funding Project of the National Key Laboratory of Biochemical Engineering(Y22504A169)the‘Strategic Priority Research Program’of the Chinese Academy of Sciences(XDA09030301-3)Beijing Natural Science Foundation(Z141100000214010).
文摘Long-circulating drug carriers are highly desirable in drug delivery system.However,nonspecific protein adsorption leaves a great challenge in drug delivery of intravenous administration and significantly affects both the pharmacokinetic profiles of the carrier and drugs,resulting in negatively affect of therapeutic efficiency.Therefore,it is important to make surface modification of drug carriers by protein-resistant materials to prolong the blood circulation time and increase the targeted accumulation of therapeutic agents.In this review,we highlight the possible mechanism of protein resistance and recent progress of the alternative protein-resistant materials and their drug carriers,such as poly(ethylene glycol),oligo(ethylene glycol),zwitterionic materials,and red blood cells adhesion.
基金supported by Military Medical Innovation Project(16CXZ032)National Science and Technology Major Projects for“Major New Drugs Innovation and Development”(No.2018ZX09J18107-03,2018ZX09721003-005-009)。
文摘The present review sets out to discuss recent developments of the effects and mechanisms of carrier properties on their circulation time.For most drugs,sufficient in vivo circulation time is the basis of high bioavailability.Drug carrier plays an irreplaceable role in helping drug avoid being quickly recognized and cleared by mononuclear phagocyte system,to give drug enough time to arrive at targeted organ and tissue to play its therapeutic effect.The physical and chemical properties of drug carriers,such as size,shape,surface charge and surface modification,would affect their in vivo circulation time,metabolic behavior and biodistribution.The final circulation time of carriers is determined by the balance between macrophage recognitions,blood vessel penetration and urine excretion.Therefore,when designing the drug delivery system,we should pay much attention to the properties of drug carriers to get enough in vivo circulation time to arrive at target site eventually.This article mainly reviews the effect of carrier size,size,surface charge and surface properties on its circulation time in vivo,and discusses the mechanism of these properties affecting circulation time.This review has reference significance for the research of long-circulation drug delivery system.
基金Supported by the National Natural Science Foundation of China (Grant No. 50573040)Major State Basic Research Development Program of China (Grant No. 2007CB935601)
文摘This paper reports on the synthesis and characterization of 4 nm magnetite nanoparticles coated with amphiphilic block copolymers of poly(ethyl methacrylate)-b-poly(2-hydroxyethyl methacrylate) (PEMA- b-PHEMA) by surface-initiated atom transfer radical polymerization (ATRP), which can act as new potential carriers for hydrophobic targeted drug delivery. Vibrating sample magnetometer analysis indi-cated that the magnetite nanoparticles were superparamagnetic at room temperature. Thermogravim-etric analysis (TGA) was applied to studying the property of surface of magnetite nanoparticles, and the surface density of macromolecules was calculated. The grafting density of oleic acid, BrMPA and PEMA was 5.8, 3.9, 0.16 chain/nm2 respectively, which indicates that the initiation efficiency decreases due to the influence of large space of oleic acid molecules. In vitro progesterone and (-)-isoproterenol hy-drochloride release in phosphate buffered saline (PBS) at pH 7.0 and 37℃ was conducted in order to demonstrate the function of drug loading and release. The results showed that the amount of drug carried into the core-shell Fe3O4@PEMA-b-PHEMA depends on the length of hydrophobic segment of block copolymer. The release of progesterone (37% after 22 h in our previous work) was compared with the release of (-)-isoproterenol hydrochloride (80% after 50 min), demonstrating that the strong hy-drophobic interaction between hydrophobic segment and drug can effectively control the release of hydrophobic drugs.
基金Supported by the Emphases Program for Science and Technology of Hunan Province (Grant No. 03NKY1001)985 Foundation Grant from Hunan University
文摘Dialdehyde starch nanoparticles (DASNP) were prepared by the redox reaction of NaIO4 and starch in water-in-oil microemulsion. IR spectrum showed that DASNP had aldehyde groups, and quantitative alkali consumption showed that its dialdehyde content was about (50±5)%. The average diameter of DASNP determined by SEM was about 100 nm. TGA-DTA showed that its thermal stability was better than starch nanoparticle (StNP) and dialdehyde starch (DAS). Its low biological toxicity was detected by cell experiment. Also the best mass ratio of doxorubicin (DOX) to combined DASNP detected by UV-VIS was 15 : 1, and the product was effective for controlled release of DOX. The cell experiment showed that the drug-carrier particle (DOX-DASNP) can release DOX for a long time and strengthened the effect of the anticancer drug. This work demonstrates that the DASNP, which has good thermal stability, small particle size, low biological toxicity, and slowly anticancer drug-releasing to strengthen drug effect, is a potentially useful carrier for anticancer drug.
基金Funded by the National Natural Science Foundation of Hubei Province(No.2014CFB306)the National Natural Science Foundation of China(No.51772233)+1 种基金the National Key Research and Development Program of China(No.2016YFC1101605)the Science and Technology Support Program of Hubei Province(No.2015BAA085)
文摘To design a new type of antitumor nanodrug carrier with good biocompatibility, a drug delivery system with a 2.19% drug-loading rate, measured by high-performance liquid chromatography(HPLC), was prepared by membrane hydration using a mixed polymer: Pluronic■ F-127, which binds folic acid(FA), Pluronic■ F-68 and triptolide(TPL)(FA-F-127/F-68-TPL). As a control, another drug delivery system based on a single polymer(FA-F-127-TPL) with a 1.90% drug-loading rate was prepared by substituting F-68 with F-127. The average particle sizes of FA-F-127/F-68-TPL and FA-F-127-TPL measured by a particle size analyzer were 30.7 nm and 31.6 nm, respectively. Their morphology was observed by atomic force microscopy(AFM). The results showed that FA-F-127-TPL self-assembled into nanomicelles, whereas FA-F-127/F-68-TPL self-assembled into nanogels. An MTT assay showed that a very low concentration of FA-F-127/F-68-TPL or FA-F-127-TPL could significantly inhibit the proliferation of multidrug-resistant(MDR) breast cancer cells(MCF-7/ADR cells) and induce cell death. The effects were significantly different from those of free TPL(P < 0.01). Using the fluorescent probe Nile red(Nr) as the drug model, FA-F-127/F-68-Nr nanogels and FAF-127-Nr nanomicelles were prepared and then incubated with human hepatocarcinoma(HepG2) and MCF-7/ADR cells, and the fluorescence intensity in the cells was measured by a multifunctional microplate reader. The results indicated that both FA-F-127/F-68-Nr and FA-F-127-Nr had sustained release in the cells, but HepG2 and MCF-7/ADR cells exhibited significantly higher endocytosis of FA-F-127/F-68-Nr than that of FA-F-127-Nr(P < 0.01). A nude mice transplanted tumor model was prepared to monitor FA-F-127/F-68-Nr in the tumor tissue and organs by whole-body fluorescent imaging. The results showed that FA-F-127/F-68-Nr targeted tumor tissues. The prepared nanogels had small particle size, were easy to swallow, exhibited slow release property,targeted tumor cells, and could improve the antitumor effects of TPL;hence, they are ideal carriers for low-dose antineoplastic drugs.
基金Supported by the Natural Science Foundation of Shandong Province (Grant No. Q2006F01)Scientific and Technological Project of Shandong Province (Grant No. 2007GG3WZ02066)+1 种基金Scientific and Technological Project of Department of Education, Shandong (Grant No. J07WC01)supported by the Key Laboratory of Bio-physics of Shandong Province
文摘One-pot synthesis of magnetic nanogels with excellent biocompatibility via the photochemical method is reported in this paper.Poly(PEGMA) modified superparamagnetic nanogels(poly(PEGMA) magnetic nanogels) were synthesized by in-situ polymerization using poly(ethylene glycol) methacrylate(PEGMA) as the monomer and N,N'-methylene-bis-(acrylamide)(MBA) as the cross-linking agent in magnetite aqueous suspension under UV irradiation.The surface functional groups and components of magnetic nanogels were analyzed by Fourier transform infrared spectroscopy(FTIR) and a thermogra-vimetric analyzer(TGA).The results indicated that the poly(PEGMA) magnetic nanogels were synthe-sized successfully by coating poly(PEGMA) on the Fe3O4 nanoparticles under UV irradiation,and the Fe3O4 nanoparticles content in this nanogels was above 50 wt%.The morphology,size,zeta-potential and magnetic property were also characterized.The magnetic nanogels had a nearly spherical shape and core-shell structure,the average size in aqueous system measured by photon correlation spec-troscopy(PCS) was 68.4 nm,which was much bigger than that in the dry state,the nanogels behaved superparamagnetically with saturated magnetization of 58.6 emu/g,and the zeta-potential was-16.3-_17.3 mV at physiological pH(6.8-7.4) which could help to maintain stability in blood.The preliminary application as drug carrier was made and the doxorubicin-loaded magnetic nanogels had an excellent property in slow-release.The experiment indicated that the magnetic nanogel was an ideal candidate carrier in target drug delivery systems and other biomedical application.
基金Supported by the National Natural Science Foundation of China (No. 29836130)
文摘Amphiphilic diblock copolymers composed of methoxy polyethylene glycol (MePEG) and poly(D,L- lactide) (PDLLA) were prepared for the preparation of polymeric micelles. The use of MePEG-PDLLA as drug carriers has been reported in the open literature, but there are only few data on the application of a se- ries of MePEG-PDLLA copolymers with different lengths in the medical field. The shape of the polymeric mi- celles is also important in drug delivery. Studies on in vitro drug release profiles require a good sink condi- tion. The critical micelle concentration of a series of MePEG-PDLLA has a significant role in drug release. To estimate their feasibility as a drug carrier, polymeric micelles made of MePEG-PDLLA block copolymer were prepared by the oil in water (O/W) emulsion method. From dynamic light scattering (DLS) measurements, the size of the micelle formed was less than 200 nm. The critical micelle concentration of polymeric micelles with various compositions was determined using pyrene as a fluorescence probe. The critical micelle con- centration decreased with increasing number of hydrophobic segments. MePEG-PDLLA micelles have a considerably low critical micelle concentration (0.4-0.5 μg/mL), which is apparently an advantage in utilizing these micelles as drug carriers. The morphology of the polymeric micelles was observed using scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The micelles were found to be nearly spherical. The yield of the polymeric micelles obtained from the O/W method is as high as 85%.
基金Supported by the National Natural Science Foundation of China (Grant No. 50372013)the Specialized Research Fund for the Doctoral Program of Higher Education of China (Grant No. 20050562002)the Guangdong Provincial Natural Science Foundation of China (Grant No. 07001769)
文摘Nano-carbon and iron composite―carbon-coated iron nanoparticles (CCINs) produced by carbon arc method can be used as a new kind of magnetic targeting induction heating drug carrier for cancer therapy. The structure and morphology of CCINs are studied by X-ray diffraction (XRD) and transmission electron microscope (TEM). Mossbauer spectra of these nanoparticles show that they contain only iron and carbon, without ferric carbide and ferric oxide. CCINs can be used as the magnetic drug carrier, with the effect of targeting magnetic induction heating in its inner core and higher drug adsorption in its nano-carbon shell outside because of its high specific surface area. CCINs can absorb Epirubicin (EPI) of 160 μg/mg measured by an optical spectrometer. In acute toxicity experiment with mice, the median lethal dose (LD50) of EPI is 16.9 mg/kg, while that of EPI-CCINs mixture is 20.7 mg/kg and none of the mice died after pure CCINs medication. The results show that pure CCINs belong to non-toxic grade and EPI delivery in mixture with CCINs can reduce its acute toxicity in mice. The magnetic properties of CCINs and their magnetic induction heating are investigated. The iron nanoparticle in its inner core has better magnetism with a good effect on targeting magnetic induction heating. When the CCINs are mixed with physiological salt water and are injected uniformly in pig's liver, the temperature goes up to 48℃. While in the case that CCINs are filled in a certain section of pig's liver, the temperature goes up to 52℃. In both cases the temperature is high enough to kill the cancer cell. CCINs have potential applications in cancer therapy.
