Tamilvanan S, Venkatesh Babu R, Kannan K, Basu S K, Sa B
Department of Pharmaceutical Sciences, University of Antwerp, 2610 Wilrijk, Antwerp, Belgium.
PDA J Pharm Sci Technol. 2008 Mar-Apr;62(2):125-54.
In the last couple of decades, use of biodegradable polymer-based microspheres has been recognized as an interesting and promising approach for parenteral controlled delivery of therapeutic peptide/protein, including antigens. The main objectives of this review are (i) to update the current state of art of manufacturing of peptide/protein-loaded microspheres through both conventional and newer microencapsulation techniques, and (ii) to bring into focus the various possible instability problems, and the investigated mechanistic ways to obviate the instability problems of peptide/protein drug during microspheres preparation as well as its release from the microspheres. The solubilization, stabilization, and preservation enhancing excipients that are used in peptide/protein-loaded microspheres are briefly overviewed.
在过去几十年中，基于可生物降解聚合物的微球已被公认为是一种用于肠胃外控制递送治疗性肽/蛋白质（包括抗原）的有趣且有前景的方法。本综述的主要目的是：（i）通过传统和新型微囊化技术，更新负载肽/蛋白质微球的制造技术现状；（ii）聚焦各种可能的不稳定性问题，以及为避免在微球制备过程中以及微球释放过程中肽/蛋白质药物的不稳定性问题而研究的机制方法。简要概述了用于负载肽/蛋白质微球的增溶、稳定和保存增强辅料。
