快速膜乳化法制备载生长激素释放肽-6的PLGA微球  

Preparation of Growth Hormone-releasing Peptide-6 Loaded PLGA Microspheres by Premix Membrane Emulsification

作　　者：何帆[1,2] 齐峰[1,2] 吴颉[1] 苏志国[1] 

机构地区：[1]中国科学院过程工程研究所生化工程国家重点实验室,北京100190 [2]中国科学院大学,北京100049

出　　处：《过程工程学报》2013年第3期458-465,共8页The Chinese Journal of Process Engineering

基　　金：国家自然科学基金委员会与香港研究资助局联合科研基金资助项目(编号:25004)

摘　　要：采用快速膜乳化法制备了聚(乳酸羟基乙酸)(PLGA)微球,得到制备PLGA微球的优化条件为:过膜压力5kPa,水相中PVA浓度19g/L,油/水相体积比1:10,该条件下所制空白微球的平均粒径约为24μm,粒径分布系数Span0.7.在此基础上制备载生长激素释放肽-6(GHRP-6)微球,油相乳化剂浓度2.5g/L、外水相中NaCl浓度10g/L条件下所制载GHRP-6微球包埋率最高可达85%,初乳制备方式对药物包埋率及体外释放行为均有较大影响,超声法制备的初乳所得微球内部结构紧密,药物包埋率较高(85%),但释药缓慢;而均质法制备的初乳所得微球内部结构疏松,药物包埋率较低(76.8%),但在体外释放更完全.Poly（lactic-co-glycolic acid） （PLGA） microspheres were prepared by premix membrane emulsification. The final optimum conditions for their particle size and size distribution were obtained： transmembrane pressure 5 kPa, concentration of poly（vinyl alcohol） in water phase 19 g/L and volume ratio of oil phase to water phase 1：10. The mean particle size of microspheres prepared under the optimal conditions was about 24 μm with Span value below 0.7. Furthermore, growth hormone-releasing peptide-6 loaded PLGA microspheres were prepared. The encapsulation efficiency of GHRP-6 loaded microspheres reached 85% under the concentration of Arlacel 83 2.5 g/L and concentration of NaC1 in external water phase 10 g/L. Primary emulsion method had significant effect on both encapsulation efficiency and in vitro release profile. The microspheres prepared by ultrasonication showed compact interior structure with high encapsulation efficiency but slow as well as incomplete drug release; in comparison, the microspheres prepared by homogenization exhibited loose structure with decreased encapsulation efficiency and constant drug release.

关 键 词：快速膜乳化 聚(乳酸-羟基乙酸)微球 粒径均一 生长激素释放肽-6 初乳制备方式 

分 类 号：R944.5[医药卫生—药剂学]