Vaginal Chitosan Tablets with Clotrimazole—Design and Evaluation of Mucoadhesive Properties Using Porcine Vaginal Mucosa, Mucin and Gelatine

Abstract

Topical administration of clotrimazole represents the common use therapy in the antimycotic genitourinary tract treatment. Due to the fast self-cleaning action of the vagina, commercially available vaginal dosage forms with clotrimazole cannot assure prolonged contact time with mucosa, therefore the main objective of this study was to develop a dosage form for vaginal administration of clotrimazole using chitosan-a biodegradable and biocompatible derivative of chitin. Tablets mucoadhesive properties were examined using texture analyser under the presence of porcine vaginal mucosa and two different models of adhesive layersmucin gel and gelatine discs. In addition, friability, hardness, swelling behaviour, residence time, surface morphology of the performed tablets, the in vitro release profile of clotrimazole and clotrimazole release kinetics were determined. The release of clotrimazole from formulations with 25 or 40% of chitosan (F2 and F3) followed non Fickian diffusion through chitosan-gel layer and was retarded up to 6 h. Additionally, tablets F2 showed the best results in terms of mucoadhesive properties and appeared to be a good alternative to commercially available antimycotic vaginal dosage forms.

A Novel Method for Preparing Surface-Modified Fluocinolone Acetonide Loaded PLGA Nanoparticles for Ocular Use: In Vitro and In Vivo Evaluations

“…The high performance of chitosan-modified/coated particles has been proved in many of them (42)(43)(44), the cationic nature of chitosan as well as its distinguished mucoadhesive properties are the main reason. Such simple modifications for nanoparticles by coating them with chitosan can ensure a prolonged drug residence time in the site of action which can guarantee the improvement of the bioavailability of drugs (45). Table VI shows the data for chitosan HCl-coated F2; the formation of a chitosan HCl layer on the surface of the nanoparticles can be confirmed by comparing the particle size as well as the zeta potential values of nanoparticles before and after chitosan HCl coating.…”

The Effect of β-Glycerophosphate Crosslinking on Chitosan Cytotoxicity and Properties of Hydrogels for Vaginal Application

“…One milliliter samples were then suitably diluted with mobile phase and analysed for CLO content by HPLC method according to [8] in the following conditions: Zorbax Eclipse XDB-C18, 4.6 mmˆ150 mm, 5 µm column (Agilent, Waldbronn, Germany); mobile phase: methanol-phosphate buffer pH 7.4 (4:1, v/v), flow rate: 1.0 mL¨min´1; UV detection at 210 nm; retention time 5.3 min; the standard calibration curve was linear over the range of 1-100 µg¨mL´1 (R 2 = 0.997).…”

“…In the recent years, mucoadhesive delivery systems providing intimate contact between a dosage form and the vaginal mucosa have gained a great attention [3,4]. Among mucoadhesive polymers, chitosan (CS) is extensively studied in designing ocular [5], buccal [6], nasal [7], and vaginal dosage forms [8,9]. In addition, CS is currently receiving great interest in pharmaceutical and biomedical fields, particularly because of its penetration enhancement capability [10,11] and antifungal activity [12][13][14].…”

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“…In contrast, the sol phase of respiratory mucus is thought to be cleared much less rapidly than the more solid-like luminal gel layer [24][25][26][27] . Continuous secretion and clearance by peristaltic forces leads to quick turnover times, on the order of 4 -6 h, in the rat GIT 7,28,29 and likely similar values in humans. In the vagina, mucus is cleared (expelled through the introitus) by intra-abdominal pressure as well as abdominal motions, which squeeze the walls of the vagina together 30,31 .…”