复乳法制备阿柔比星A的聚乳酸聚乙醇酸共聚物纳米粒影响包封率因素考察  

Effect of experimental parameters on the encapsulation of aclarubicin Aloaded PLGA nanoparticles prepared by a double emulsion method

作　　者：陈蜀[1] 张志荣[1] 石海涛[1] 卢颖名[1] 

机构地区：[1]四川大学华西药学院,成都610041

出　　处：《中国抗生素杂志》2005年第6期338-340,共3页Chinese Journal of Antibiotics

摘　　要：以含阿柔比星A(AclarubicinA,ACRB-A)的酸性溶液为内水相,采用复乳法制备ACRB-A(PLGA)纳米粒。考察了有机溶剂、油酸的量、稳定剂种类、投药量、乳化剂、Na2SO4的量和外水相的pH值几个主要因素对ACRB-APLGA纳米粒包封率的影响。结果表明,以二氯甲烷和丙酮为有机溶剂、油酸(15mg)、右旋糖酐-70、ACRB-A的浓度(5mg/ml)、以F68和Tween-80为乳化剂、2%的Na2SO4和外水相的pH等于8有利于提高ACRB-A的包封率。经实验条件优化后制备的ACRB-APLGA包封率为85.41%,纳米粒粒径为272nm,粒径分散指数为0.213。Aclarubicin A (ACRB-A) loaded poly (DL-lactide-co-glycolic acid) (PLGA) nanoparticles (ACRB-A-PLGA-NPs) were prepared with a double emulsion method (W/O/W), using acid solution containing ACRB-A as inner water phase. Experimental parameters including the organic solvent, the concentration of oleic acid, the kinds of stabilizer, the concentration of the ACRB-A and Na_2SO_4, and the pH of the outer water phase were investigated for the encapsulation efficiency. The results showed that the improvement of the incorporation efficiency of ACRB-A contributed to the following factors: acetone and dichloromethane used as (organic) solvent, F68 and Tween-80 as emulsifier, oleic acid (15mg), Dextran-70, ACRB-A (5mg/ml), Na_2SO_4 (2%), pH8.0 of outer water phase. Optimized preparation parameters lead to the successful preparation of nanoparticles characterized with encapsulation efficiency up to 85.41%, size 272nm and particle dispersibility index (PDI) 0.213.

关 键 词：阿柔比星A PLGA 纳米粒 包封率 

分 类 号：R944.9[医药卫生—药剂学]