Drug Discov Ther. 2009;3(1):6-9.

Formulation and evaluation of in situ gelling thermoreversible mucoadhesive gel of fluconazole.

Gonjari ID, Hosmani AH, Karmarkar AB, Godage AS, Kadam SB, Dhabale PN

The purpose of the present study was to develop ophthalmic gel formulations of fluconazole. Intraocular delivery of topically applied drugs such as fluconazole is hampered by elimination of the solution due to tear turnover, so an in situ gelling thermoreversible mucoadhesive gel was formulated. Thermoreversible mucoadhesive gels were prepared using the cold method along with poloxamer 407 and different mucoadhesive polymers such as hydroxy ethyl cellulose (HEC), hydroxy propyl methyl cellulose (HPMC) K4M, and polyvinyl pyrrolidone (PVP) K30. Gels were evaluated for physical parameters like appearance, gelation temperature, pH, spreadability, drug content, gel strength, bioadhesion, and in vitro permeation. A modified device (modified K-C diffusion cell with a sheep's eye corneal membrane as a diffusion membrane) was used for evaluation of drug permeation through a sheep's corneal membrane. The formulated gels were transparent, uniform in consistency, and had spreadability with a pH range of 6.8 to 7.3. Satisfactory bioadhesion on the sheep's corneal surface and good gel strength were also observed. Diffusion studies have shown that a matrix is the best-fit model. As the concentration of mucoadhesive agent increases, the rate of permeation decreases. The order of drug permeation through the membrane was HEC > PVP K30 > HPMC K4M. This study found that a thermoreversible polymer and mucoadhesive polymers can be effectively used to prolong residence time.

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