膜乳化法与复乳法结合制备粒径均一的载溶菌酶微胶囊

Preparation of Uniform-sized PLA/PLGA Microcapsules Containing Lysozyme by Combining Porous Glass Membrane Emulsification and Multiple Emulsion-solvent Evaporation

采用微孔膜乳化法与复乳法结合制备粒径均一可控的以聚乳酸和聚(乳酸-羟基乙酸)共聚物为膜材的载溶菌酶微胶囊,粒径分布系数CV(CoefficientofVariation)为14.04%,远低于机械搅拌法制备的微囊的CV(76.54%).分别加入内水相添加剂PVA,PEG400,HP-β-CD,使溶菌酶的包埋率从无添加剂时的68.1%分别增大到86.6%,89.0%和94.1%.添加剂降低了溶菌酶的突释.PEG400,PEG6000,HP-β-CD的加入降低了溶菌酶的释放速率,而PVP或PVA的加入则加快了溶菌酶的释放.溶菌酶在油水界面上的吸附变性是失活的主要原因.在酶液中加入PEG400,PEG6000,PVP,HP-β-CD可有效地避免由于油水界面造成的溶菌酶活性的损失.

Relatively uniform-sized biodegradable poly（lactide） （PLA） and poly（lactide-co-glycolide） （PLGA） microcapsules containing lysozyme were successfully prepared by combining porous glass membrane emulsification technique with multiple emulsion-solvent evaporation method. Compared with the stirring method, it was found that the sizes of microcapsules are more uniform, the coefficient of variation （CV） value which indicates the size distribution was 14.04%. It was found that adding additives to inner aqueous phase could efficiently improve the drug encapsulation efficiency, adjust the drug release profile and maintain the bioactivity of drug. When PVA, PEG400 and HP-β-CD were separately added into the inner aqueous phase, the encapsulation efficiency increased from 68.1% to 86.6%, 89.0% and 94.1% respectively, The cumulative release amount was decreased when PEG400, PEG6000, HP-β-CD were added. While it was enhanced when PVP or PVA was added. It demonstrated that the main reason for protein deactivation was lysozyme adsorption onto the W1/O interface. The loss of lysozyme activity was successfully prevented by adding PEG400, PEG6000, HP-β-CD or PVP into the inner aqueous phase.