Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 365, Issue 1-2, Pages 143-149Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2008.08.004
Keywords
Cyclosporine A; Microemulsion; In situ gelling system; Kelcogel (R); Ophthalmic delivery
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Funding
- National High Technology Research and Development Program of China [2007AA021604]
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The objective of the present study was to design a novel microemulsion in situ electrolyte-triggered gelling system for ophthalmic delivery of a lipophilic drug, cyclosporine A (CsA). A CsA-loaded microemulsion was prepared using castor oil, Solutol HS 15 (surfactant), glycerol and water. This microemulsion was then dispersed in a Kelcogel (R) solution to form the final microemulsion in situ electrolyte-triggered gelling system. In vitro, the viscosity of the CsA microemulsion Kelcogel (R) system increased dramatically on dilution with artificial tear fluid and exhibited pseudo-plastic rheology. In vivo results revealed that the AUC(0-->32h) of corneal CsA for the microemulsion Kelcogel (R) system was approximately three-fold greater than for a CsA emulsion. Moreover, at 32 h after administration, CsA concentrations delivered by the microemulsion Kelcogel (R) system remained at therapeutic levels in the cornea. This CsA microemulsion in situ electrolyte-triggered gelling system might provide an alternative approach to deliver prolonged precorneal residence time of CsA for preventing cornea allograft rejection. Published by Elsevier B.V.
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