Cho S W, Song S H, Choi Y W
Department of Pharmaceutics, College of Pharmacy, Chung-Ang University, Seoul, Korea.
Arch Pharm Res. 2000 Aug;23(4):385-90. doi: 10.1007/BF02975452.
To demonstrate the effect of formulation conditions on the controlled release of protein from poly(lactide-co-glycolide) (PLGA) microspheres for use as a parenteral drug carrier, ovalbumin (OVA) microspheres were prepared using the W/O/W multiple emulsion solvent evaporation and extraction method. Methylene chloride or ethyl acetate was applied as an organic phase and poly(vinyl alcohol) as a secondary emulsion stabilizer. Low loading efficiencies of less than 20% were observed and the in vitro release of OVA showed a burst effect in all batches of different microspheres, followed by a gradual release over the next 6 weeks. Formulation processes affected the size and morphology, drug content, and the controlled release of OVA from PLGA microspheres.
为证明制剂条件对用作肠胃外药物载体的聚(丙交酯-乙交酯)(PLGA)微球中蛋白质控释的影响,采用水包油包水多重乳液溶剂蒸发和萃取法制备了卵清蛋白(OVA)微球。使用二氯甲烷或乙酸乙酯作为有机相,聚乙烯醇作为二次乳液稳定剂。观察到负载效率低于20%,并且在所有不同批次的微球中,OVA的体外释放均呈现突释效应,随后在接下来的6周内逐渐释放。制剂工艺影响了PLGA微球的大小和形态、药物含量以及OVA的控释。