丹皮酚聚乳酸羟基乙酸微球的制备及体外释药考察

Preparation and in vitro Release Behavior of Paeonol PLGA Microspheres

目的:制备丹皮酚聚乳酸羟基乙酸(PLGA)微球,考察其体外释药过程。方法:以丹皮酚为芯材,以PLGA为载体,采用乳化溶剂挥发法制备丹皮酚PLGA微球;以聚乙烯醇质量分数、PLGA质量浓度、药物与PLGA质量比及水油相体积比为考察因素,以包封率和载药量的综合评分为评价指标,采用正交试验优选制备工艺;扫描电镜和光学显微镜观察微球的外观和粒径,并测定其体外释药过程。结果:优选的工艺为聚乙烯醇质量分数0.9%、PLGA质量浓度60g/L、药物与PLGA质量比1∶3、水油相体积比1∶10。制得的微球球型规则,表面平滑,平均粒径为(31.75±0.13)μm。微球的载药量为(21.16±0.51)%,包封率为(66.91±1.62)%,8h体外累积释药量为37%。结论:所选工艺可用于制备丹皮酚PLGA微球,可为缓释药物传递系统的开发提供参考。

OBJECTIVE ： To prepare Paeonol PLGA microspheres, and to investigate the process of drug release. METHODS： PLGA microspheres loaded with paeonol were prepared by emulsion/solvent evaporation method using paeonol as core materials and PLGA as wall materials. The preparation technology was optimized by orthogonal test with mass fraction of PVA, mass concen- tration of PLGA,ratio of drug to PLGA,volume ratio of water to oil as factors using encapsulation rate and drug-loading amount as index. The surface morphology and structure and drug release behavior were all observed. RESULTS：The optimized technology was as follows： mass fraction of PVA was 0.9 %, mass concentration of PLGA wes 60 g/L, ratio of drug to PLGA was 1 ： 3, volume ratio of water to oil was 1 ： 10. Prepared microspheres was regular spherical in shape, smooth in appearance. Average particle size was （31.75 ± 0.13） μm, drug-loading amount was （21.16 ± 0.51）%, encapsulation rate was（66.91 ± 1.62）%, and accumulative release amount was 37% in 8 h. CONCLUSIONS：The technology be used for the preparation of Paenol PLGA microspheres and can provide reference for the development of sustained-release drug delivery system.