微球中聚乳酸羟基乙酸共聚物浓度与微球结构、释药、降解的关系研究

发布时间：2018-07-10 01:38

本文选题：微球 + 聚乳酸羟基乙酸共聚物　；参考：《中国药房》2015年07期

【摘要】：目的:研究微球中聚乳酸羟基乙酸共聚物(PLGA)浓度与微球结构、释药、降解的关系。方法:以牛血清白蛋白(BSA)为药物,采用复乳法制备PLGA浓度分别为10%、15%、20%的BSA-PLGA微球,以包封率、载药量、粒径为指标考察PLGA浓度对3种微球性质的影响;采用扫描电子显微镜观察3种微球和降解40 d内的外观和内部形态;使用荧光蛋白-异硫氰酸荧光素牛血清白蛋白代替BSA作为模型药物制备PLGA微球,并采用激光共聚焦显微镜观察荧光蛋白在微球骨架内的分布情况;采用BCA法考察3种微球的体外释药情况;采用压汞仪考察降解28 d内20%PLGA所制微球的孔径、孔隙率、截面孔隙率的变化;采用凝胶渗透色谱法检测10%、20%PLGA所制微球降解28 d内分子质量及其降解模型拟合。结果:与10%、15%PLGA所制微球比较,20%PLGA所制微球的包封率[(81.96±1.84)%]和粒径[(139.50±0.21)μm]最大,载药量[(7.28±0.45)%]最低,截面孔隙率[(32.35±1.98)%]和孔径[(12.43±0.14)μm]最小,释药突释率最低,40 d内的释放速率相对较慢,降解后截面孔隙率最大,降解均遵循假一级模式(r2=0.065 3)。结论:在考察范围内,随着PLGA浓度的增加,微球的结构更致密,释药更平稳,降解更易形成中空结构。
[Abstract]:Aim: to study the relationship between the concentration of poly (lactic acid) glycolic acid (PLGA) and the structure, drug release and degradation of microspheres. Methods: bovine serum albumin (BSA) was used to prepare BSA-PLGA microspheres with the concentration of 10% and 15% respectively. The effects of PLGA concentration on the properties of the three microspheres were investigated by encapsulation efficiency, drug loading and particle size. The appearance and internal morphology of three kinds of microspheres were observed by scanning electron microscope (SEM), and the PLGA microspheres were prepared by using fluorescent protein-fluorescein isothiocyanate bovine serum albumin (BSA) instead of BSA as model drug. The distribution of fluorescent protein in microspheres was observed by laser confocal microscopy, the drug release of three microspheres in vitro was investigated by BCA method, and the pore size and porosity of the microspheres prepared by PLGA within 28 days after degradation were examined by mercurimeter. The molecular weight and degradation model of the microspheres prepared by 10 and 20 PLGA were determined by gel permeation chromatography within 28 days. Results: the encapsulation efficiency and particle size of microspheres [(81.96 卤1.84)%] and diameter [(139.50 卤0.21) 渭 m] were the highest, the drug loading [(7.28 卤0.45)%] was the lowest, the cross section porosity [(32.35 卤1.98)%] and pore size [(12.43 卤0.14) 渭 m] were the lowest, and the release rate of drug release was relatively slow in 40 days. After degradation, the porosity of the cross section was the largest, and the degradation followed the pseudo-first-order model (r 20.065 3). Conclusion: with the increase of PLGA concentration, the structure of microspheres is denser, the drug release is more stable, and the degradation is easier to form hollow structure.
【作者单位】：中山大学附属第三医院;中山大学药学院;
【分类号】：R944

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