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 Shigeru Itai Shuji Noguchi Yasunori Iwao
• 来源期刊: 药理与制药(英文)
• 学科: 医学
• 关键词: Poly-Lactic-Co-Glycolic-Acid Microparticle Suppression of INITIAL Burst Release Coating Bovine Serum Albumin
• 年，卷（期）: ylyzyyw_2013,（8）
• 页码范围: 578-583
• 页数: 6页
• 分类号: R73

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.