期刊
CORNEA
卷 33, 期 1, 页码 77-81出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/ICO.0b013e3182a7f3bf
关键词
surfactant micelles; cyclosporin A; poor solubility; dry eye disease; bioavailability
资金
- Bavarian Research Foundation [BFS AZ 870-90]
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.
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