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Comparative Study
. 2008;9(3):953-65.
doi: 10.1208/s12249-008-9132-y. Epub 2008 Aug 16.

Effect of thiolated polymers to textural and mucoadhesive properties of vaginal gel formulations prepared with polycarbophil and chitosan

Erdal Cevher  1 , Demet Sensoy, Mohamed A M Taha, Ahmet Araman
Affiliations
Comparative Study

Effect of thiolated polymers to textural and mucoadhesive properties of vaginal gel formulations prepared with polycarbophil and chitosan

Erdal Cevher et al. AAPS PharmSciTech. 2008.

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 micromol 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.

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Figures

Fig. 1
Fig. 1
FT-IR spectrums of a polycarbophil and polycarbophil–cystein conjugate and b chitosan and chitosan–thioglycolic acid conjugate
Fig. 2
Fig. 2
Hardness of the gel formulations (n = 6)
Fig. 3
Fig. 3
Compressibility of the gel formulations (n = 6)
Fig. 4
Fig. 4
Elasticity of the gel formulations (n = 6)
Fig. 5
Fig. 5
Cohesiveness of the gel formulations (n = 6)
Fig. 6
Fig. 6
Adhesiveness of the gel formulations (n = 6)
Fig. 7
Fig. 7
Work of mucoadhesion of the gel formulations (n = 6)
Fig. 8
Fig. 8
In vitro drug release profiles of CLM from the gel formulations including a polycarbophil and polycarbophil–cystein conjugate and b chitosan and chitosan–thioglycolic acid conjugate (n = 3)
Fig. 9
Fig. 9
Stability graph of CLM in a PG-CYS6 and b CHI-TGA6 formulations
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