Effect of Thiolated Polymers to Textural and Mucoadhesive Properties of Vaginal Gel Formulations Prepared with Polycarbophil and Chitosan


Cevher E., Sensoy D., Taha M. A. M., Araman A.

AAPS PHARMSCITECH, vol.9, no.3, pp.953-965, 2008 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 9 Issue: 3
  • Publication Date: 2008
  • Doi Number: 10.1208/s12249-008-9132-y
  • Journal Name: AAPS PHARMSCITECH
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.953-965
  • Keywords: chitosan-thioglycolic acid, clomiphene citrate, gel, human papilloma virus, polycarbophil-cysteine, texture profile analysis, vaginal mucoadhesion, DRUG-DELIVERY SYSTEMS, IN-VITRO EVALUATION, MECHANICAL CHARACTERIZATION, INSITU HYBRIDIZATION, PERIODONTAL-DISEASE, LIQUID SUPPOSITORY, BIOADHESIVE, BIOAVAILABILITY, RELEASE, DESIGN
  • Istanbul University Affiliated: Yes

Abstract

The aim of this study was to design and evaluate of mucoadhesive gel formulations for the vaginal application of clomiphene citrate (CLM) for local treatment of human papilloma virus (HPV) infections. Chitosan (CHI) and polycarbophil (PC) were covalently modified using the thioglycolic acid and L-cysteine, respectively. The formation of thiol conjugates of chitosan (CHI-TG) and polycarbophil (PC-CYS) were confirmed by FT-IR analysis and PC-CYS and CHI-TG were found to have 148.42 +/- 4.16 and 41.17 +/- 2.34 mu mol of thiol groups per gram of polymer, respectively. One percent CLM gels were prepared by combination of various concentrations of PC and CHI with thiolated conjugates of these polymers. Hardness, compressibility, elasticity, adhesiveness and cohesiveness of the gels were measured by Texture profile analysis and the vaginal mucoadhesion was investigated by mucoadhesion test. The increasing in the amount of the thiol conjugates was found to enhance the elasticity, cohesiveness, adhesiveness and mucoadhesion of the gel formulations but not their hardness and compressibility when compared to gels prepared using their respective parent formulations. Slower release rate of CLM from gels was achieved when the polymer concentrations were increased in the gel formulations. PC and its thiol conjugate were found to prolong the release of CLM longer than 70 h unlike gel formulations prepared using CHI and its thiol conjugate which were able to release CLM up to 12 h. Stability of CLM was preserved during the 3 month stability analysis under controlled room temperature and accelerated conditions.