Department of Drug and Food Control, Faculty of Pharmacy, Tehran University of Medical Science Tehran, Tehran, Iran.
Pharm Res. 2024 Apr;41(4):765-778. doi: 10.1007/s11095-024-03682-6. Epub 2024 Mar 19.
Biodegradable polyesters are widely employed in the development of controlled release systems for peptide drugs. However, one of the challenges in developing a polyester-based delivery system for peptides is the acylation reaction between peptides and polymers. Peptide acylation is an important factor that affects formulation stability and can occur during storage, in vitro release, and after drug administration. This review focuses on the mechanisms and parameters that influence the rate of peptide acylation within polyesters. Furthermore, it discusses reported strategies to minimize the acylation reaction.
可生物降解的聚酯在肽类药物的控释系统的开发中被广泛应用。然而，在开发基于聚酯的肽类药物传递系统时，面临的挑战之一是肽与聚合物之间的酰化反应。肽酰化是影响制剂稳定性的一个重要因素，它可能发生在储存、体外释放和药物给药后。本文综述了影响聚酯中肽酰化速率的机制和参数，并讨论了减少酰化反应的报道策略。
