目的:优化BSA-PLGA微球制备工艺,并对其包封率、形态、体外释放药物及微球包裹前后BSA的稳定性进行评价.方法:以PLGA为载体,采用复乳溶剂挥发法制备BSA-PLGA微球.Micro BCA法测定微球的包封率和载药量,扫描电子显微镜观察微球的形态,激光粒度仪测定粒度及分布,聚丙烯酰胺凝胶电泳(SDS-PAGE)研究微球包裹前后BSA分子结构的完整性,同时考察体外释药性能.结果:根据优化工艺制备的微球外观圆整,平均粒径(2275.8±256.9)nm,包封率(82.59±2.92)%,载药量(13.76±0.49)×10~(-2)%,包裹前后BSA结构稳定,体外释放28天以上,释放曲线符合Higuchi方程.结论:本研究获得了较优化的BSA-PLGA微球制备工艺,所制备的微球具有较高的包封率和明显的缓释效果.
To optimize the preparation procedure of bovine serum albumin-poly(lactic-co-glycolide acid)(BSA-PLGA)microspheres and to evaluate its encapsulation efficiency,morphology,release in vitro and the stability of BSA before and after incorporating,BSA-PLGA microspheres were prepared by using the(water-in-oil)-in-water double-emulsion solvent evaporation technique,in which PLGA was used as the encapsulation material.The loading capacity and encapsulation efficiency of BSA in the microspheres were determined by micro-bicinchoninic acid(BCA)assay.Scanning electron microscopy(SEM)was used for the observation of microspheres.Size distribution was determined by laser scattering technique.The integrity of BSA was evaluated by sodium dodecyl sulphate-polyacrylamide gel electrophoresis(SDS-PAGE).The release in vitro of microspheres was examined.Microspheres prepared under optimum conditions had regular morphology.The average particle size was 2275.8±256.9 nm,while the encapsulation efficiency and the drug loading were (82.59±2.92)% and(13.76±0.49)×10~(-2)%,respectively.SDS-PAGE experiments suggested that incorporated BSA was stable.The sustained release in vitro could last for more than 28 days and the release profiles conformed to the Higuchi equation.Optimized preparation process of BSA-PLGA microspheres with a relatively high encapsulation efficiency and an obvious sustained release activity in vitro are obtained in this study.
参考文献
| [1] | Hariharan S;Bhardwaj V;Bala I;Sitterberg J;Bakowsky U;Ravi Kumar MN .Design of estradiol loaded PLGA nanoparticulate formulations: a potential oral delivery system for hormone therapy.[J].Pharmaceutical research,2006(1):184-195. |
| [2] | van-de-Weert M;Hennink WE;Jiskoot W .Protein instability in poly(lactic-co-glycolic acid) microparticles.[J].Pharmaceutical research,2000(10):1159-1167. |
| [3] | Kim HK;Park TG .Comparative study on sustained release of human growth hormone from semi-crystalline poly(L-lactic acid) and amorphous poly(D,L-lactic-co-glycolic acid) microspheres: morphological effect on protein release[J].Journal of Controlled Release: Official Journal of the Controlled Release Society,2004(1):115-125. |
| [4] | 徐希明,沈玉萍,余江南,皋古云,曹建平.聚乳酸-聚乙二醇共聚物为载体的缓释疫苗微球的制备及特性研究[J].中国药学杂志,2005(14):1080-1082. |
| [5] | 刘世芸,徐超,冯乙巳,宋礼华.白蛋白聚乳酸缓释微球的制备及体外释放研究[J].合肥工业大学学报（自然科学版）,2006(12):1584-1587. |
| [6] | Cui F;Cun DM;Tao AJ;Yang MS;Shi K;Zhao M;Guan Y .Preparation and characterization of melittin-loaded poly (DL-lactic acid) or poly (DL-lactic-co-glycolic acid) microspheres made by the double emulsion method[J].Journal of Controlled Release: Official Journal of the Controlled Release Society,2005(2):310-319. |
| [7] | Mao S;Xu J;Cai C;Germershaus O;Schaper A;Kissel T .Effect of WOW process parameters on morphology and burst release of FITC-dextran loaded PLGA microspheres.[J].International Journal of Pharmaceutics,2007(1/2):137-148. |
| [8] | Yang YY.;Chung TS.;Chia HH. .Effect of preparation temperature on the characteristics and release profiles of PLGA microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method[J].Journal of Controlled Release: Official Journal of the Controlled Release Society,2000(1):81-96. |
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