Evaluation of chitosan based vaginal bioadhesive gel formulations for antifungal drugs

Abstract

Vaginal yeast infections are among the most common reasons for women seeking medical care; it has been estimated that 70-75 % of women have an episode of Candida vaginitis at least once during their lifetime (1). Local administration of antimicrobial agents has been favored in the treatment of vaginitis because of the numerous side effects of systemically applied drugs. Vaginal dosage forms used for this purpose include solutions, gels, creams, ointments, foams, pessaries, tablets and vaginal inserts (1). To achieve a desirable therapeutic effect, vaginal delivery systems need to have the ability to spread onto the vaginal mucosa surface and guarantee an intimate and prolonged contact at the site of application (2). Therefore, localized mucoadhesive dosage forms The aim of the present study was to evaluate chitosan as a vaginal mucoadhesive gel base for econazole nitrate and miconazole nitrate. To this aim, different types of chitosan with different molecular masses and viscosity properties [low molecular mass chitosan (viscosity: 20,000 mPa s), medium molecular mass chitosan (viscosity: 200,000 mPa s), high molecular mass chitosan (viscosity: 800,000 mPa s)] have been used. First, rheological studies were conducted on chitosan gels. Mechanical, syringeability and mucoadhesive properties of chitosan gels were determined. Release profiles of econazole nitrate and miconazole nitrate from chitosan gels were obtained and evaluated kinetically. In addition, anticandidal activities of formulations were determined. Finally, vaginal retention of chitosan gels in rats was evaluated by in vivo distribution studies. Based on the results, it can be concluded that gels prepared with medium molecular mass chitosan might be effectively used for different antifungal agents in the treatment of vaginal candidiosis, since it has high mucoadhesiveness, suitable mechanical and release properties with good vaginal retention.

Utilization of nanotechnology to enhance percutaneous absorption of acyclovir in the treatment of herpes simplex viral infections

“…This may be explained by the increase in molecular weight of chitosan leading to increased viscosity of the obtained hydrogel, which decreases the spreadability of the hydrogel, in agreement with previous work. 29 The same finding was observed with regard to the effect of concentration of chitosan (X 2 ) on spreadability. When the concentration of chitosan (X 2 ) increased from 1% to 3% in the formulations with the same level of the other factors, the spreadability (Y 1 ) of the hydrogel decreased from 4.1 in F2 to 3.0 in F11, from 3.2 in F3 to 2.9 in F12, and from 4.0 in F5 to 3.6 in F8.…”

Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan–thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers

“…According to the literature and pre-formulation studies, 18,43 chitosan of high molecular weight at a concentration of 2% was identified as the most suitable vehicle for intravesical administration of NPs, because significant increase in the work of mucoadhesion was observed as the molecular weight and viscosity of chitosan increased.…”

“…18 The gel was left at 25°C until a clear solution was obtained, and then NPs were dispersed in chitosan gel.…”

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“…In addition to binding to the surface of Caco-2 cells and human enterocytes, WGA is also taken up into the cells by receptor mediated endocytosis involving the epidermal growth factor (EGF) receptor, which is present in a significant amount even on enterocytes. Poly(lactide-co-glycide) (PLGA) NPs conjugated with WGA as a carbohydrate binding ligand showed improved cytoassociation as compared to the unmodified ones 19,27,46 .…”