雌二醇聚乳酸类微囊的制备与体外评价

目的　以聚乳酸或乳酸 乙醇酸共聚物为载体材料制备雌二醇缓释微囊。方法　实验中采用乳化 溶剂萃取法制备微囊 ,考察了影响微囊特性以及体外释药的各种因素 ,采用单因素试验方差分析进行因素影响的显著性检验 ,并在此基础上采用T方法进行两两间多重比较 ,进一步考察因素各水平间差异的显著性。结果　结果表明 ,粒径和加水萃取速度对雌二醇微囊的包封率有显著性影响 (P <0 0 1) ;随油相载体的浓度以及加水萃取速度对微囊的粒径影响显著 (P <0 0 1)。体外释药研究表明 ,加水萃取速度和载体的型号和分子量对微囊释药影响显著 (P <0 0 1)。但这些影响因素的各水平之间的差异性并不都具有显著性。结论　通过改变处方以及制备工艺可以得到具有不同性质的雌二醇聚乳酸类缓释微囊

Preparation and in Vitro Evaluation of Polylactiv Acid (PLA) or Polylactic-co-Glycolic Acid (PLGA) Microcapsules Loaded with Estradiol

Aim PLA/PLGA was used as biodegradable and biocompatible carriers to achieve sustained release of estradiol (E 2). Methods Microcapsules (MC) were prepared by an emulsification solvent extraction method, and then the properties and in vitro drug release behavior of MC were examined. An analysis of variance (ANOVA) was used to test the statistical significance. Then, multiple comparisons were made with a T method between levels to examine the significance of difference further. For all the results a P value >0 05 was considered statistically insignificant . Results Under the same conditions, the water adding speed and the particle size had significant effects ( P <0 01) on the entrapment efficiency of MC; the water adding speed and the concentration of PLA in the oil phase had significant effects ( P <0 01) on the diameter MC in medium. Release of E 2 from MC was influenced significantly ( P <0 01) by the water adding speed and the type and molecule weight of the polymers. But the differences between levels of the variates were not all significant. Conclusion E 2 PLA/PLGA MC with various properties can be formed when the formulation and the technology were changed accordingly.