State Key Laboratory of Biochemical Engineering, Institute of Process Engineering, Chinese Academy of Sciences, Beijing, China.
University of Chinese Academy of Sciences, Beijing, China.
J Microencapsul. 2022 Aug;39(5):452-466. doi: 10.1080/02652048.2022.2100934. Epub 2022 Jul 28.
Gonadotropin-releasing hormone (GnRH) agonists are peptides consisting of nine or ten amino acid residues. GnRH agonists have been applied in the therapy of sexual hormone disorders like prostate cancer, endometriosis, uterine myoma, central precious puberty, and in-vitro fertility. Treatment is achieved by continuous hormone intake and long-term agonists administration, which is usually associated with poor patient compliance. Because GnRH agonists that are administered with the parenteral route are broken down by peptidase, their half-life is short. As a result, developing sustained release for the drug delivery system is significant. Even though some drugs have been successfully delivered with long-acting release microspheres and approved by the Food and Drug Administration (FDA), some challenges remain. This review highlighted current approaches to encapsulate GnRH agonists into delivery systems and strategies encountered during the loading process. Moreover, the following sections provide strategies to improve the release profile, and animal and human studies were summarised.
促性腺激素释放激素（GnRH）激动剂是由九个或十个氨基酸残基组成的肽。GnRH 激动剂已应用于治疗性甾体激素紊乱，如前列腺癌、子宫内膜异位症、子宫肌瘤、中枢性性早熟和体外受精。治疗方法是持续摄入激素和长期使用激动剂，这通常与患者的依从性差有关。由于通过肠外途径给予的 GnRH 激动剂被肽酶分解，因此其半衰期短。因此，开发用于药物递送系统的持续释放是非常重要的。尽管一些药物已经通过长效释放微球成功递送并获得美国食品和药物管理局（FDA）的批准，但仍存在一些挑战。本综述强调了当前将 GnRH 激动剂封装到递送系统中的方法以及在加载过程中遇到的策略。此外，以下部分提供了改善释放特性的策略，并总结了动物和人体研究。
