Clotrimazole nanoparticle gel for mucosal administration

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• 作者：Elisabetta Esposito^a ; ^ese@unife.it ; Laura Ravani^a ; Catia Contado^b ; Andrea Costenaro^a ; Markus Drechsler^c ; Damiano Rossi^d ; Enea Menegatti^a ; Alessandro Grandini^d ; Rita Cortesi^a
• 关键词：Nanostructured lipid carriers ; Cubosome ; Poloxamer gel ; Sedimentation Field Flow Fractionation ; Candidosis
• 刊名：Materials Science and Engineering: C
• 出版年：2013
• 出版时间：1 January, 2013
• 年：2013
• 卷：33
• 期：1
• 页码：411-418
• 全文大小：1260 K

文摘

In this study a formulation suitable to be applied on oral and/or vaginal mucosa has been developed for the treatment of fungal infections.

The aim of the research is a comparison between clotrimazole (CLO) containing semisolid formulations based on monoolein aqueous dispersion (MAD) or nanostructured lipid carrier (NLC). MAD and NLC have been characterized in terms of morphology and dimensional distribution by cryogenic Transmission Electron Microscopy (cryo-TEM) and Photon Correlation Spectroscopy (PCS). CLO was encapsulated with high entrapment efficiency both in MAD and in NLC, according to Sedimentation Field Flow Fractionation (SdFFF) combined with HPLC. CLO recovery in MAD and NLC has been investigated by time.

In order to obtain formulations with suitable viscosity for mucosal application, MAD was diluted with a carbomer gel, while NLC was directly viscosized by the addition of poloxamer 407 in the dispersion. The rheological properties of MAD and NLC after viscosizing have been investigated.

Franz cell has been employed to study CLO diffusion from the different vehicles, evidencing diffusion rates from MAD and NLC superimposable to that obtained using Canesten^?.

An anticandidal activity study demonstrated that both CLO-MAD and CLO-NLC were more active against Candida albicans with respect to the pure drug.