Exploring the Therapeutic Potential of Cyclosporine for Ophthalmic Indications by Novel Carrier Systems

Crit Rev Ther Drug Carrier Syst. 2023;40(5):1-45. doi: 10.1615/CritRevTherDrugCarrierSyst.2022043085.

Abstract

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.

Publication types

  • Review

MeSH terms

  • Administration, Ophthalmic
  • Cyclosporine* / chemistry
  • Cyclosporine* / therapeutic use
  • Drug Delivery Systems
  • Excipients
  • Eye
  • Eye Diseases* / drug therapy
  • Humans
  • Immunosuppressive Agents / therapeutic use

Substances

  • Cyclosporine
  • Immunosuppressive Agents
  • Excipients