Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research-Ahmedabad (NIPER-A), Gandhinagar, Gujarat 382355, India.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad, India.
Crit Rev Ther Drug Carrier Syst. 2023;40(5):1-45. doi: 10.1615/CritRevTherDrugCarrierSyst.2022043085.
Cyclosporine (CsA) stays the most intangible molecule holding a good history for treating several ophthalmic conditions and it even attributes to multiple off-label uses. Topical delivery of CsA is the most preferred route but owing to the molecule's physicochemical properties such as poor aqueous solubility and high molecular weight as well as its encounter with multiple barriers of eye causes hindrance for proper delivery of the molecule to the site of action. However, Restasis®, Cequa®, and Verkazia® are the marketed formulations that have been approved by U.S. Food and Drug Administration, whereas Cyclokat® and Ikervis® by the European Medicines Agency. Although these medications are in use, they are associated with severe discomfort and poor patient compliance. This review gives an overview regarding current formulations available in the market, the products in pipeline and the recent advances undertaken for improving ocular delivery of CsA for various ophthalmic indications.
环孢素(CsA)是一种最有效的分子,在治疗多种眼科疾病方面有着良好的历史,甚至具有多种非适应证用途。局部给药是最受欢迎的途径,但由于该分子的物理化学性质,如低水溶性和高分子量,以及它在眼部遇到的多种障碍,导致该分子不能正确递送到作用部位。然而,Restasis®、Cequa®和Verkazia®是已经被美国食品和药物管理局批准的上市制剂,而 Cyclokat®和 Ikervis®则是被欧洲药品管理局批准的制剂。尽管这些药物在使用中,但它们会引起严重的不适和较差的患者依从性。本综述概述了目前市场上可获得的制剂、正在研发的产品以及为改善各种眼科适应证中环孢素的眼内递药而进行的最新进展。