Romanian Society of Pharmaceutical Sciences

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CHITOSAN/HPMC-BASED HYDROGELS CONTAINING ESSENTIAL OILS FOR TOPICAL DELIVERY OF FLUCONAZOLE: PRELIMINARY STUDIES

ANA MARIA MUŢ 1#, LAVINIA VLAIA 1#*, GEORGETA CONEAC 1#, IOANA OLARIU 1#, VICENŢIU VLAIA 1#, CORINA STĂNCIULESCU 2#, MIRELA ADRIANA MITU 3#, ZOLTAN SZABADAI 4#, DUMITRU LUPULIASA 3#

1.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, 2 Eftimie Murgu Square, 300041, Timişoara, Romania
2.“Victor Babeş” University of Medicine and Pharmacy, Faculty of Medicine, 2 Eftimie Murgu Square, 300041, Timişoara, Romania
3.“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, 8 Traian Vuia Street, Bucharest, Romania
4.National Institute for Research and Development in Electrochemistry and Condensed Matter, 114 Dr. Aurel Păunescu Podeanu Street, Timişoara, Romania
*corresponding author: vlaia.lavinia@umft.ro
#All authors had equal contribution.

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Among the pharmaceutical excipients of natural origin, polysaccharides (i.e. chitosan and cellulose derivatives) and essential oils have attracted increasing interest as gelling agents and penetration enhancers respectively, for development of topical semisolid preparations, including hydrogels. Therefore, in this research an attempt has been made to design and prepare new biocompatible hydrogels, using fluconazole (FZ) as model drug, two mixed polysaccharides (chitosan and hydroxypropylmethylcellulose) as gelling agents, clove oil (CVO) and cinnamon oil (CNO) as potential penetration enhancers and synergistic antifungal components, cosolvents and a non-ionic synthetic surfactant as solubilizers. The prepared hydrogels were characterized for drug content, pH and rheological properties (flow behaviour, viscosity, consistency and spreadability). Also, in vitro fluconazole release through hydrophilic synthetic membrane was evaluated by vertical diffusion cell method. The obtained results revealed that all experimental formulations were homogeneous, with adequate rheological characteristics and possessed pH values very close to the lower limit of the compendial range. Based on the obtained results, it can be suggested that both essential oil composition and its concentration in the formulations have significant effects on the mechanical properties and pharmaceutical availability of the tested hydrogels. In vitro drug release results sustained that the most desirable topical vehicles for fluconazole delivery, the formulations FZ-CNO 3%, FZ-CNO 5% and FZ-CVO 5%, containing 3% or 5% cinnamon oil and respectively 5% clove oil incorporated into a chitosan-hydroxypropylmethylcellulose based hydrogel. In conclusion, these hydrogels should be further investigated by in vitro and in vivo studies as promissing carriers for topical fluconazole delivery.