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A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca

Authors Jerkins GW, Pattar GR, Kannarr SR

Received 21 August 2019

Accepted for publication 31 January 2020

Published 20 February 2020 Volume 2020:14 Pages 481—489

DOI https://doi.org/10.2147/OPTH.S228070

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4

Editor who approved publication: Dr Scott Fraser


Gary W Jerkins,1 Guruprasad R Pattar,2 Shane R Kannarr3

1Advancing Vision Research, Nashville, TN, USA; 2The Eye Care Institute, Louisville, KY, USA; 3Kannarr Eye Care, Pittsburg, KS, USA

Correspondence: Gary W Jerkins
Advancing Vision Associates, 4306 Harding Pike, Nashville, TN 37205, USA
Tel +1 615 502-2871
Email drjeyeguy@garyjerkins.com

Abstract: Keratoconjunctivitis sicca (KCS) is a multifactorial disease characterized by tear hyperosmolarity, inflammation, and ocular surface damage. Cyclosporine A (CsA) is used as an effective disease-modifying agent to improve the signs and symptoms of KCS by reducing inflammation, which interferes with tear production. This review provides an overview of efficacy, safety, and limitations of currently marketed topical CsA formulations—including CsA ophthalmic emulsion, cationic nanoemulsion, and aqueous nanomicelles—and highlights newer technologies for controlled ocular delivery of CsA and their clinical implications. Long available emulsion formulations of CsA are oil-based and have several limitations, including slow onset of efficacy and low intraocular penetration and bioavailability. Aqueous CsA nanomicelle carriers produce rapid improvement in objective signs of KCS such as corneal and conjunctival staining as early as 4 weeks and have acceptable safety profiles. CsA formulations using semifluorinated alkanes or polyaphrons are currently in clinical development, having recently completed Phase 2 studies. Other carriers for CsA currently in the preclinical phase include microemulsions, polymeric aqueous and lyophilized micelles, and hydrogels; these novel formulations have yet to undergo clinical trials. Formulations that improve tissue availability of CsA may be beneficial in clinical practice by providing faster onset of relief and improving patient adherence.

Keywords: cyclosporine A, keratoconjunctivitis sicca, emulsion, nanomicelles, OTX-101

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