4.4 Article

Evaluation of Glycofurol-Based Gel as a New Vehicle for Topical Application of Naproxen

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AAPS PHARMSCITECH
卷 11, 期 3, 页码 1138-1146

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SPRINGER
DOI: 10.1208/s12249-010-9485-x

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glycofurol; naproxen; permeation coefficient; physical stability; skin irritation test; topical delivery

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In view of the good skin tolerability, glycofurol was used as a vehicle-based gel, and its effect in the topical penetration of Naproxen (NAP) was investigated. The aims of this study were to develop a suitable gel with bioadhesive property, spreadability, and viscosity for topical anti-inflammatory effect. Three gelling and adhesive agents were examined: Carbopol 974P, Gantrez AN 119, and polyvinylpyrollidone K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell in order to optimize the gel formulation. The permeation rate of NAP-based gel across the excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (J(ss)), permeability coefficient (K-p), and penetration index (PI) was observed in optimized formulation containing 2% Transcutol as an permeation enhancer. From skin irritation test, it was concluded that the optimized novel glycofurol-based gel formulation was safe to be used for topical drug delivery. The developed glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.

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