盐酸米诺环素复合微球的制备及其性能检测

Preparation and performance of minocycline hydrochloride composite microspheres

目的:用聚乳酸乙醇酸共聚物-高分子脂质体核壳(PLGA-Liposome)纳米粒制备牙周缓释制剂盐酸米诺环素复合微球,并检测体外释放和相关性能。方法:采用复乳法-薄膜分散法制备盐酸米诺环素-聚乳酸乙醇酸共聚物-高分子脂质体核壳复合微球(MH-PLGA-Liposome),以MH-PLGA为对照,比较两种微球的形貌,粒径及其体外释放等特性。结果:两组微球均为球形;粒径均为纳米级,MH-PLGA-Liposome组大于MH-PLGA组(P<0.05);MH-PLGA/Liposome表面带正电荷;其6h累积释放量为15.8%,显著小于对照组29%,突释明显减低且有长效缓释作用。结论:PLGA/Liposome载药体系具有显著减少突释的性能和更好的缓释效果。

AIM ： To develop a new drug carrier system of nanoparticles of mixed liposome monolayer shell and biodegradable PLGA core for delivery of minocycline hydrochloride （ MH ） and measure its properties in vitro. METHODS：The morphology, size and drug release of MH-PLGA/Liposome, prepared by double emulsion -film dis- pelion method, was compared with a control group of MH-PLGA in vitro. RESULTS： Both groups of microspheres were of spherical shape and of Manometer grade in size. The size of MH-PLGA/Liposome microspheres was larger than that of MH-PLGA microspheres （P 〈0.05）. MH-PLGA/Liposome had positive electric charge, decreased burst re- lease （only 15.8% release in the first 6 hours） and prolonged MH release time. CONCLUSION： Our results show that the PLGA/liposomes drug carrier system has little burst release, good sustained releasing effect and it may be a useful drug delivery system.