One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins

作     者：Hiroyuki Takabe Moriyuki Ohkuma Yasunori Iwao Shuji Noguchi Shigeru Itai 

作者机构：Department of Pharmaceutical Engineering Graduate School of Pharmaceutical Sciences University of Shizuoka Shizuoka Japan. Drug Formulation Department Central Research Laboratories Kaken Pharmaceutical Co. Ltd. Shizuoka Japan Drug Formulation Department Central Research Laboratories Kaken Pharmaceutical Co. Ltd. Shizuoka Japan Department of Pharmaceutical Engineering Graduate School of Pharmaceutical Sciences University of Shizuoka Shizuoka Japan. 

出 版 物：《Pharmacology & Pharmacy》 (药理与制药（英文）)

年 卷 期：2013年第4卷第8期

页      面：578-583页

学科分类：1002[医学-临床医学] 100214[医学-肿瘤学] 10[医学] 

主　　题：Poly-Lactic-Co-Glycolic-Acid Microparticle Suppression of Initial Burst Release Coating Bovine Serum Albumin 

摘      要：An initial burst is often observed during the release of active pharmaceutical ingredients (APIs) from poly-lactic-coglycolic-acid (PLGA) microparticles (MPs) which have been prepared by the emulsion-solvent evaporation method. Herein, we describe the development of a simple one-step coating method that suppresses the initial burst release process. This new method involves coating the PLGA-MPs with PLGA, with the coating process being performed through the phase separation of PLGA on the surface of PLGA-MPs using the emulsion-solvent evaporation method. Bovine serum albumin (BSA) was encapsulated in the PLGA-MPs as a model API. The coated MPs were spherical in shape with no pores on their smooth surface, whereas the non-coated PLGA-MPs had porous surfaces. An in vitro release study showed that the residual levels of BSA in the coated and non-coated PLGA-MPs after 1 h were about 99% and 16% of the original loads, respectively. The one-step coating method therefore represents a useful method for preparing PLGA-MPs that do not give an initial burst release of proteinaceous APIs.