A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca
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, USACorrespondence: Gary W JerkinsAdvancing Vision Associates, 4306 Harding Pike, Nashville, TN 37205, USATel +1 615...
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2020-02-01
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| Series: | Clinical Ophthalmology |
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| Online Access: | https://www.dovepress.com/a-review-of-topical-cyclosporine-a-formulationsmdasha-disease-modifyin-peer-reviewed-article-OPTH |
| _version_ | 1818739148892143616 |
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| author | Jerkins GW Pattar GR Kannarr SR |
| author_facet | Jerkins GW Pattar GR Kannarr SR |
| author_sort | Jerkins GW |
| collection | DOAJ |
| description | 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, USACorrespondence: Gary W JerkinsAdvancing Vision Associates, 4306 Harding Pike, Nashville, TN 37205, USATel +1 615 502-2871Email drjeyeguy@garyjerkins.comAbstract: 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 |
| first_indexed | 2024-12-18T01:20:14Z |
| format | Article |
| id | doaj.art-6acca0bd8bf949c6aafde28f313d065a |
| institution | Directory Open Access Journal |
| issn | 1177-5483 |
| language | English |
| last_indexed | 2024-12-18T01:20:14Z |
| publishDate | 2020-02-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Clinical Ophthalmology |
| spelling | doaj.art-6acca0bd8bf949c6aafde28f313d065a2022-12-21T21:25:50ZengDove Medical PressClinical Ophthalmology1177-54832020-02-01Volume 1448148951974A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis SiccaJerkins GWPattar GRKannarr SRGary 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, USACorrespondence: Gary W JerkinsAdvancing Vision Associates, 4306 Harding Pike, Nashville, TN 37205, USATel +1 615 502-2871Email drjeyeguy@garyjerkins.comAbstract: 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-101https://www.dovepress.com/a-review-of-topical-cyclosporine-a-formulationsmdasha-disease-modifyin-peer-reviewed-article-OPTHcyclosporine akeratoconjunctivitis siccaemulsionnanomicellesotx-101 |
| spellingShingle | Jerkins GW Pattar GR Kannarr SR A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca Clinical Ophthalmology cyclosporine a keratoconjunctivitis sicca emulsion nanomicelles otx-101 |
| title | A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca |
| title_full | A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca |
| title_fullStr | A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca |
| title_full_unstemmed | A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca |
| title_short | A Review of Topical Cyclosporine A Formulations—A Disease-Modifying Agent for Keratoconjunctivitis Sicca |
| title_sort | review of topical cyclosporine a formulations mdash a disease modifying agent for keratoconjunctivitis sicca |
| topic | cyclosporine a keratoconjunctivitis sicca emulsion nanomicelles otx-101 |
| url | https://www.dovepress.com/a-review-of-topical-cyclosporine-a-formulationsmdasha-disease-modifyin-peer-reviewed-article-OPTH |
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