New Frontiers Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan; Bioengineering Laboratory, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
New Frontiers Research Laboratories, Toray Industries, Inc., 6-10-1 Tebiro, Kamakura, Kanagawa 248-8555, Japan.
J Control Release. 2014 Jan 10;173:89-95. doi: 10.1016/j.jconrel.2013.10.035. Epub 2013 Nov 4.
A reverse polymer micelle with a diameter of 100nm was prepared for a protein carrier releasing payloads in a pH-dependent manner. The reverse polymer micelle was made from an amphiphilic diblock copolymer of biodegradable poly(d,l-lactic-co-glycolic acid) (PLGA) and biocompatible poly(ethylene glycol) (PEG). PLGA having a terminal carboxyl group was additionally embedded in the micelle's PLGA layer via hydrophobic interaction. The micelles encapsulating bovine serum albumin and streptavidin released the proteins under neutral and basic conditions, whereas the proteins remained in the interior at acidic pH. Using erythropoietin as a protein drug, it was also exemplified that the released protein retained its cell proliferation activity even after rigorous formulation processes, including water-in-oil emulsion. The present reverse polymer micelle could potentially find application as an oral protein drug delivery carrier.
一种直径为 100nm 的反向聚合物胶束被制备出来，用作一种蛋白质载体，以 pH 依赖性方式释放有效载荷。该反向聚合物胶束由可生物降解的聚（D，L-乳酸-共-乙醇酸）（PLGA）和生物相容性聚（乙二醇）（PEG）的两亲性嵌段共聚物组成。具有末端羧基的 PLGA 通过疏水相互作用进一步嵌入胶束的 PLGA 层中。包封牛血清白蛋白和链霉亲和素的胶束在中性和碱性条件下释放蛋白质，而在酸性 pH 下蛋白质保留在内部。使用促红细胞生成素作为蛋白质药物的实例表明，即使经过包括油包水乳液在内的严格制剂工艺处理，释放的蛋白质仍保留其细胞增殖活性。这种新型反向聚合物胶束可能有潜力作为口服蛋白质药物传递载体。
