Luschmann, C. and Herrmann, W. and Strauss, O. and Luschmann, K. and Goepferich, A. (2013) Ocular delivery systems for poorly soluble drugs: An in-vivo evaluation. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 455 (1-2). pp. 331-337. ISSN 0378-5173,
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For highly potent but poorly water-soluble drugs like cyclosporine A, the development of aqueous formulations providing an increase of corneal drug tissue levels, and thus of bioavailability, to increase patient compliance is still a challenge. Therefore, we designed two water-based liquid application systems, an in-situ nanosuspension (INS) and a micellar solution (MS), and tested both formulations in vivo at the rabbit cornea for tolerability and the tissue uptake of CsA. The evaluation of the biological tolerability by periodical eye examination during 180 min and quantification in a defined grading system revealed that the INS evoked minimal to no irritations whereas the MS was perfectly tolerated. After the observation period, the rabbits were sacrificed and the corneal tissue levels of CsA were analyzed. The INS and the MS both showed high levels of 1683 +/- 430ngng(CsA)/g(cornea) and 826 +/- 163ng(CsA)/g(cornea), respectively, and exceeded drug tissue levels reported for Restasis (R) (350ng(CsA)/g(cornea)) and cationic emulsions (750ng(CsA)/g(cornea)). These results marked our INS and MS as outstanding novel approaches for the treatment of inflammatory corneal diseases. Copyright (C) 2013 Elsevier B.V. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DRY EYE DISEASE; CYCLOSPORINE-A; PENETRATION; FORMULATION; RABBITS; Surfactant micelles; In-situ nanosuspension; Cyclosporine A; Dry eye disease; Biocompatibility; Bioavailability |
| Subjects: | 600 Technology > 610 Medical sciences Medicine 600 Technology > 615 Pharmacy |
| Divisions: | Medicine > Lehrstuhl für Augenheilkunde Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Technology (Prof. Göpferich) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 31 Mar 2020 09:39 |
| Last Modified: | 31 Mar 2020 09:39 |
| URI: | https://pred.uni-regensburg.de/id/eprint/15845 |
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