Univ Paris Sud, UMR CNRS 8612, IFR 141, Faculté de Pharmacie, Châtenay-Malabry, France.
Expert Opin Drug Deliv. 2012 Mar;9(3):343-54. doi: 10.1517/17425247.2012.662484. Epub 2012 Feb 16.
Thanks to recent advances in biotechnology, the use of peptides and proteins as drugs has become a concrete clinical reality, and consequently an interesting challenge has emerged for non-parenteral drug delivery. Leuprolide is a synthetic nonapeptide agonist to the luteinizing hormone-releasing hormone (LH-RH) receptor with principal clinical applications for prostate cancer. Although a large number of formulations available, they mainly consist in depot subcutaneous injections or implantable devices. Both of these routes of administration present multiple limitations considering the large clinical applications of this active substance.
The objective of this review is to critically discuss the formulations currently available on the market for leuprolide optimization and to consider how drug delivery plays an important role in improving the bioavailability of this compound.
Due to its physicochemical properties and its economical market, leuprolide is an interesting candidate for drug delivery to improve the efficacy of existing treatments, dose adjustments, and patient compliance and safety.
得益于生物技术的最新进展，肽和蛋白质作为药物的应用已成为现实，因此非肠道药物输送面临着有趣的挑战。亮丙瑞林是促黄体激素释放激素（LH-RH）受体的合成九肽激动剂，主要用于前列腺癌。尽管有大量的制剂可用，但它们主要包括皮下储库注射或可植入装置。考虑到这种活性物质的大量临床应用，这两种给药途径都存在多种局限性。
本文的目的是批判性地讨论目前市场上用于优化亮丙瑞林的制剂，并考虑药物输送如何在提高该化合物的生物利用度方面发挥重要作用。
由于其物理化学性质和经济市场，亮丙瑞林是改善现有治疗效果、剂量调整、患者依从性和安全性的药物输送的一个有趣的候选物。
