摘要
目的以聚乳酸-羟基乙酸共聚物为载体制备用于连接于人工晶体的金雀异黄素微球。方法采用改良的乳化溶剂挥发法制备金雀异黄素微球,应用星点设计-效应面法优化处方,以动态透析法评价微球的体外释放。结果以水相与油相的比值和聚乙烯醇浓度为考察因素,以包封率、载药量和粒径为考察指标进行处方优化,结果表明二次多项式拟合的效果较好,较优的处方为聚乙烯醇浓度0.88%;水相与油相的比值为6.46。通过优化处方制得的微球形态圆整,包封率、载药量、平均粒径分别为73.72%、6.70%和34.21μm,与方程预测值的偏差分别为1.25%、1.33%和7.81%,微球体外168 h累计释放率达64.53%。结论本试验建立的处方优化模型预测性良好,制得的金雀异黄素微球具有良好的理化性质,并且满足长效缓释的要求。
Objective To develop genistein-loaded sustained-release microspheres with poly （lactic-co-glycolic acid） （PLGA） for intraocular lens. Methods Genistein-loaded PLGA microspheres were prepared by modified emulsion- solvent evaporation method. Central composite design/response surface methodology was used to optimize the for- mulation and technology. Dynamic dialysis was used to determine the microsphere in vitro release characteristics. Results The effect of independent variables （the ratio of aqueous phase and oil phase, PVA concentration） on the response variables （encapsulation efficiency, drug loading and particle diameter） was determined by multiple linear re- gression and second-order polynomial equation. A second-order polynomial equation was used for the data and the op- timum formulation was aqueous phase to oil phase ration of 6.46 and 0.88% PVA. Spherical microspheres of smooth surface were obtained under these conditions. The encapsulation efficiency, drug loading and particle diameter were 73.72%, 6.70% and 34.21 μm. The bias between the predicted and the observed values was 1.25%, 1.33% and 7.81% respectively. The cumulative release rate of genistein-loaded PLGA microspheres was 64.53% for 168 h. Conclusion Genistein-loaded sustained-release microspheres are successfully prepared, and the optimum mathematic model is highly predictive.
出处
《中南药学》
CAS
2015年第7期689-692,共4页
Central South Pharmacy
基金
国家自然科学基金(No.81100654)
作者简介
张琦，女，硕士，主要从事药物新技术研究，Tel：13504920603，E-mail：zhangqi19881019@163．com
通讯作者：潘卫三，男，博士，教授，博士研究生导师，主要从事药物新剂型与新技术的研究，Tel：（024）23986313，E-mail：ppwwss@163．com
