Bilati Ugo, Allémann Eric, Doelker Eric
School of Pharmacy, University of Geneva, Geneva, Switzerland.
Eur J Pharm Biopharm. 2005 Apr;59(3):375-88. doi: 10.1016/j.ejpb.2004.10.006.
This paper reviews the major factors that are closely involved in peptide and protein degradation during the preparation of biodegradable nano- and microparticles. The various means usually employed for overcoming these obstacles are described, in order to bring to the fore the strategies for protein stabilization. Both processing and formulation parameters can be modified and are distinctly considered from a strategic point of view. We describe how partial or full protein stability retention within the carriers and during drug release might be achieved by individual or combined optimized strategies. Additionally, problems commonly encountered during protein quantification, stability determination and release are briefly reviewed. Artefacts that might occur during sampling and analytical procedures and which might hinder critical interpretation of results are discussed.
本文综述了在可生物降解纳米颗粒和微粒制备过程中与肽和蛋白质降解密切相关的主要因素。描述了通常用于克服这些障碍的各种方法，以突出蛋白质稳定化策略。加工和制剂参数均可修改，并从战略角度进行了明确考量。我们描述了如何通过单独或组合的优化策略在载体内部以及药物释放过程中实现部分或全部蛋白质稳定性的保留。此外，还简要回顾了蛋白质定量、稳定性测定和释放过程中常见的问题。讨论了在采样和分析过程中可能出现的、可能妨碍对结果进行关键解读的假象。
