NOVEL TOPICAL CHITOSAN/HYDROXYPROPYLMETHYLCELLULOSE
– 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#
1“Victor Babeş” University of Medicine and Pharmacy, Faculty of Pharmacy, 2 Eftimie Murgu Square, Timişoara, Romania
2“Victor Babeş” University of Medicine and Pharmacy, Faculty of Medicine, 2 Eftimie Murgu Square, Timişoara, Romania
3“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, 6 Traian Vuia Street, Bucharest, Romania
*corresponding author: vlaia.lavinia@umft.ro
#All authors have equal contribution to this paper.
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Abstract:
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/HPMCbased
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.

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