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NOVEL TOPICAL CHITOSAN/HYDROXYPROPYLMETHYL-CELLULOSE – BASED HYDROGELS CONTAINING FLUCONAZOLE AND SUCROSE ESTERS. FORMULATION, PHYSICOCHEMICAL CHARACTERIZATION, IN VITRO DRUG RELEASE AND PERMEATION

ANA MARIA MUŢ ^1#, LAVINIA VLAIA ^1#*, GEORGETA CONEAC ^1#, IOANA OLARIU ^1#, VICENŢIU VLAIA ^1#, CĂLIN POPOIU ^2#, MIRCEA HÎRJĂU ^3#, DUMITRU LUPULIASA ^3#

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The purpose of this work was to formulate, prepare and evaluate novel topical hydrogels for the fluconazole delivery, containing biocompatible, biodegradable, non-toxic, non-irritating excipients which have inherent antifungal activity, considering that a synergistic therapeutic effect can be obtained. Fluconazole (FZ) and two non-ionic natural surfactants of sucrose esters group (sucrose laurate, sucrose palmitate) as potential penetration enhancers were incorporated into a hydrogel vehicle prepared using a mixture of two biopolymers as gelling agents (chitosan and hydroxypropylmethylcellulose, HPMC). The experimental hydrogels were evaluated for physicochemical properties (drug content, pH and viscosity) and in vitro drug release through hydrophilic synthetic membrane. Also, ex vivo FZ permeation test using excised pig ear skin was performed in order to investigate the penetration enhancement effect of the two sucrose esters. Franz diffusion cells method was used in the drug release and permeation experiments. The resulted data indicated that all tested hydrogels fulfilled the official requirements regarding drug content, pH and viscosity. High flux and release rate values obtained for all FZ chitosan/HPMC-based hydrogels in the in vitro drug release study indicate the formulations performance. Based on the ex vivo drug permeation data, sucrose laurate can be considered an effective penetration enhancer for fluconazole, encouraging additional in vitro and in vivo investigations.