Luschmann, Christoph and Tessmar, Joerg and Schoeberl, Simon and Strauss, Olaf and Luschmann, Karl and Goepferich, Achim (2014) Self-Assembling Colloidal System for the Ocular Administration of Cyclosporine A. CORNEA, 33 (1). pp. 77-81. ISSN 0277-3740, 1536-4798
Full text not available from this repository. (Request a copy)Abstract
Purpose:In this study, we developed a self-assembling micellar system to deliver cyclosporine A (CsA) in an aqueous solution to the cornea.Methods:Two nonionic surfactants of the poly(ethylene glycol)-fatty alcohol ether type (Sympatens AS and Sympatens ACS) were characterized in terms of micelle size, shape, and charge, and their encapsulation efficiency for CsA. In an in situ single dose bioavailability study, the corneal CsA levels were determined in an enucleated porcine eye model. A commercial formulation and a 2% CsA olive oil solution served as references.Results:Both surfactants formed spherical micelles with a size of 9 to 12 nm in water. A concentration as low as 0.3% (wt/vol) Sympatens AS was sufficient to entrap therapeutic levels of at least 0.1% (wt/vol) CsA. In the porcine in situ model, exceptionally high drug levels in the cornea were obtained for the micellar CsA solution (1557 407 ng(CsA)/g(cornea)). They were significantly higher than those of Restasis (545 +/- 137 ng(CsA)/g(cornea)) or the olive oil solution (452 +/- 142 ng(CsA)/g(cornea)).Conclusions:In conclusion, we have shown a promising simple and efficient approach for the application of CsA in an aqueous solution to the cornea to treat inflammatory corneal diseases.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | EYE; DELIVERY; PENETRATION; DRUGS; VIVO; NANOSUSPENSION; FORMULATIONS; MICELLES; RABBITS; surfactant micelles; cyclosporin A; poor solubility; dry eye disease; bioavailability |
| Subjects: | 600 Technology > 610 Medical sciences Medicine 600 Technology > 615 Pharmacy |
| Divisions: | Medicine > Lehrstuhl für Hals-Nasen-Ohren-Heilkunde Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Technology (Prof. Göpferich) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 02 Dec 2019 14:44 |
| Last Modified: | 02 Dec 2019 14:44 |
| URI: | https://pred.uni-regensburg.de/id/eprint/11116 |
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