【正】Objective:To preliminarily investigate three different lipid matrices consisting of two natural homolipids from Capra hircus(goat fat) and Bovine Spp.(tallow fat) and one semi-synthetic lipid(Softisan~? 142) sep...【正】Objective:To preliminarily investigate three different lipid matrices consisting of two natural homolipids from Capra hircus(goat fat) and Bovine Spp.(tallow fat) and one semi-synthetic lipid(Softisan~? 142) separately structured with Phospholipon~? 90G(P90G) as potential delivery systems for poorly water soluble drugs.Methods:The structured lipid matrices were characterized by differential scanning calorimetry(DSC) and employed to prepare solid lipid microparticles(SLMs) by the melt homogenization method using gradient concentrations of polysorbate 80 and at different emulsification times of 2,5 and 10 min using a Silverson mixer. The SLMs were analyzed for morphology and particle size,thermal properties,stability studies and determination of injectability.Results:The results showed that SLM production was optimum at 5%of lipid matrices,1.5%of polysorbate 80 and emulsification time of 5 min.Increase in polysorbate 80 concentrations decreased the particle size of the SLMs.The SLMs were well formed, spherical,smooth and non-porous with particle sizes in the ranges of(13.90±2.10)μm -(0.09±0.01)μm for SLMs produced from the structured - tallow fat;(13.40±1.30)μm-(0.10±0.01)μm for the structured - goat fat and(13.40±2.00)μm-(2.10±1.00)μm for the structured Softisan~? 142 lipid matrices.DSC traces showed that Softisan~? 142 was the most crystalline of all three bulk matrices due to its high enthalpy(-7.962 mW/mg) while tallow fat was the least(-5.067 mW/mg) but addition of P90G to the matrices lowered their enthalpies mostly in the structured goat fat matrices.The SLMs when stored at 4-6°C were most stable and syringeable with 27 G needle.Conclusions:This suggests that structured goat fat matrices with the enthalpy of -2.813 mW/mg will mosdy favour drug loading of some poorly soluble drugs more than tallow fat(-4.892 mW/mg) and Softisan? 142(-5.501 mW/mg).展开更多
Objective:The effectiveness of the slimy substance in snail to regenerate and repair damaged areas on it body/shell lead to this investigation.Methods:The anti-ulcer’property of snail slime extracted from phylur moll...Objective:The effectiveness of the slimy substance in snail to regenerate and repair damaged areas on it body/shell lead to this investigation.Methods:The anti-ulcer’property of snail slime extracted from phylur mollusca(tropical snail) from the giant African snail Archachatina marginata(Fam.Arionidae) was investi gated using histamine,stress and indomethacin-induced ulcers.The solubility profile of extract was investiga ted in different solvents and at different temperatures.Chemical analysis was carried out to determine the type of constituents present in the slim,while acute toxicity test was carried out to evaluate its profile of toxicity The effect of the snail slim on gastrointestinal motility was investigated in mice,while the guinea pig ileum wa used to study the effect of the extract on contraction produced by acetylcholine and histamine.The snail slim contained copious quantity of protein,with varying amounts of simple sugars,carbohydrates and fats.Th slime was not soluble in most common solvents and increases in temperature,did not appear to increase its sol ubility.Results:The result further indicated that although the snail slime exhibited significant(P【0.05) an ti -ulcer induced by stress and histamine,it was most potent against ulcer induced by indomethacin.The snai slime potently inhibited gastrointestinal movement in mice in a dose-dependent manner;however,it was not a ble to inhibit contraction induced by acetylcholine and histamine in guinea pig ileum.Conclusion:The snai mucin possesses potent antiulcer properties without any toxic effect.The mechanism responsible for the anti-ul cer property may not be postulated with certainty but cytoprotective and anti-spasmodic activities are most likel to be involved.展开更多
Objective:To investigate the characteristics of PEGylated mucin and its potential usage. Methods:Mucin was extracted from giant African land snails and PECylated mucin was prepared with different ratios of PEG 2000-Mw...Objective:To investigate the characteristics of PEGylated mucin and its potential usage. Methods:Mucin was extracted from giant African land snails and PECylated mucin was prepared with different ratios of PEG 2000-Mwt and mucin（1:1,0:1,2:1,1:3 and 3:1 to form batch A-E） using solvent technique.The physicochemical properties of mucin were identified and the solubility of mucin was assessed.The thermal properties of PEGylated mucin were measured by differential scanning calorimetry（DSC）.Results:Carbohydrates,proteins and trace amounts of fats were present in snail mucin.The mucin powder was water-soluble at 30℃and more water-soluble at 35℃but not soluble;in acetone,ethanol,0.1 M NaOH,0.1M H<sub>2</sub>SO<sub>4</sub> and 0.1 NH<sub>4</sub>OH was water-soluble.The melting point T<sub>m</sub> ranged from 58.58℃to 61.17℃, crystallization temperature Tc 37.08℃to 39.83℃,and glass transition temperature Tg 126.85℃to 138.39℃.The variation in T<sub>m</sub>,T<sub>c</sub>,and T<sub>g</sub> with the composition in the PEGylaton showed that an interaction between PEG and mucin occured.Conclusions:This result can serve as a basis for further evaluation of the PEGylation method and be used for drug delivery.展开更多
文摘【正】Objective:To preliminarily investigate three different lipid matrices consisting of two natural homolipids from Capra hircus(goat fat) and Bovine Spp.(tallow fat) and one semi-synthetic lipid(Softisan~? 142) separately structured with Phospholipon~? 90G(P90G) as potential delivery systems for poorly water soluble drugs.Methods:The structured lipid matrices were characterized by differential scanning calorimetry(DSC) and employed to prepare solid lipid microparticles(SLMs) by the melt homogenization method using gradient concentrations of polysorbate 80 and at different emulsification times of 2,5 and 10 min using a Silverson mixer. The SLMs were analyzed for morphology and particle size,thermal properties,stability studies and determination of injectability.Results:The results showed that SLM production was optimum at 5%of lipid matrices,1.5%of polysorbate 80 and emulsification time of 5 min.Increase in polysorbate 80 concentrations decreased the particle size of the SLMs.The SLMs were well formed, spherical,smooth and non-porous with particle sizes in the ranges of(13.90±2.10)μm -(0.09±0.01)μm for SLMs produced from the structured - tallow fat;(13.40±1.30)μm-(0.10±0.01)μm for the structured - goat fat and(13.40±2.00)μm-(2.10±1.00)μm for the structured Softisan~? 142 lipid matrices.DSC traces showed that Softisan~? 142 was the most crystalline of all three bulk matrices due to its high enthalpy(-7.962 mW/mg) while tallow fat was the least(-5.067 mW/mg) but addition of P90G to the matrices lowered their enthalpies mostly in the structured goat fat matrices.The SLMs when stored at 4-6°C were most stable and syringeable with 27 G needle.Conclusions:This suggests that structured goat fat matrices with the enthalpy of -2.813 mW/mg will mosdy favour drug loading of some poorly soluble drugs more than tallow fat(-4.892 mW/mg) and Softisan? 142(-5.501 mW/mg).
文摘Objective:The effectiveness of the slimy substance in snail to regenerate and repair damaged areas on it body/shell lead to this investigation.Methods:The anti-ulcer’property of snail slime extracted from phylur mollusca(tropical snail) from the giant African snail Archachatina marginata(Fam.Arionidae) was investi gated using histamine,stress and indomethacin-induced ulcers.The solubility profile of extract was investiga ted in different solvents and at different temperatures.Chemical analysis was carried out to determine the type of constituents present in the slim,while acute toxicity test was carried out to evaluate its profile of toxicity The effect of the snail slim on gastrointestinal motility was investigated in mice,while the guinea pig ileum wa used to study the effect of the extract on contraction produced by acetylcholine and histamine.The snail slim contained copious quantity of protein,with varying amounts of simple sugars,carbohydrates and fats.Th slime was not soluble in most common solvents and increases in temperature,did not appear to increase its sol ubility.Results:The result further indicated that although the snail slime exhibited significant(P【0.05) an ti -ulcer induced by stress and histamine,it was most potent against ulcer induced by indomethacin.The snai slime potently inhibited gastrointestinal movement in mice in a dose-dependent manner;however,it was not a ble to inhibit contraction induced by acetylcholine and histamine in guinea pig ileum.Conclusion:The snai mucin possesses potent antiulcer properties without any toxic effect.The mechanism responsible for the anti-ul cer property may not be postulated with certainty but cytoprotective and anti-spasmodic activities are most likel to be involved.
文摘Objective:To investigate the characteristics of PEGylated mucin and its potential usage. Methods:Mucin was extracted from giant African land snails and PECylated mucin was prepared with different ratios of PEG 2000-Mwt and mucin（1:1,0:1,2:1,1:3 and 3:1 to form batch A-E） using solvent technique.The physicochemical properties of mucin were identified and the solubility of mucin was assessed.The thermal properties of PEGylated mucin were measured by differential scanning calorimetry（DSC）.Results:Carbohydrates,proteins and trace amounts of fats were present in snail mucin.The mucin powder was water-soluble at 30℃and more water-soluble at 35℃but not soluble;in acetone,ethanol,0.1 M NaOH,0.1M H<sub>2</sub>SO<sub>4</sub> and 0.1 NH<sub>4</sub>OH was water-soluble.The melting point T<sub>m</sub> ranged from 58.58℃to 61.17℃, crystallization temperature Tc 37.08℃to 39.83℃,and glass transition temperature Tg 126.85℃to 138.39℃.The variation in T<sub>m</sub>,T<sub>c</sub>,and T<sub>g</sub> with the composition in the PEGylaton showed that an interaction between PEG and mucin occured.Conclusions:This result can serve as a basis for further evaluation of the PEGylation method and be used for drug delivery.
