Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2009;10(2):476-81.
doi: 10.1208/s12249-009-9233-2. Epub 2009 Apr 21.

Microemulsion-based vaginal gel of clotrimazole: formulation, in vitro evaluation, and stability studies

Yogeshwar G Bachhav  1 , Vandana B Patravale
Affiliations

Microemulsion-based vaginal gel of clotrimazole: formulation, in vitro evaluation, and stability studies

Yogeshwar G Bachhav et al. AAPS PharmSciTech. 2009.

Abstract

The objective of the present investigation was to develop and evaluate microemulsion-based gel for the vaginal delivery of clotrimazole (CMZ). The solubility of CMZ in oils and surfactants was evaluated to identify components of the microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. Various gelling agents were evaluated for their potential to gel the CMZ microemulsion without affecting its structure. The bioadhesive potential and antifungal activity of the CMZ microemulsion-based gel (CMZ-MBG) was determined in comparison to the marketed clotrimazole gel (Candid-V gel) by in vitro methods. The chemical stability of CMZ in CMZ-MBG was determined as per the International Conference on Harmonization guidelines. The CMZ microemulsion exhibited globule size of 48.4 nm and polydispersity index of 0.75. Carbopol ETD 2020 could successfully gel the CMZ microemulsion without disturbing the structure. The CMZ-MBG showed significantly higher (P < 0.05) in vitro bioadhesion and antifungal activity as compared to that of Candid-V gel. The stability studies indicated that CMZ undergoes acidic pH-catalyzed degradation at all the storage conditions at the end of 3 months.

PubMed Disclaimer

Figures

Fig. 1
Fig. 1
Apparatus used for in vitro bioadhesion study
Fig. 2
Fig. 2
Ternary-phase diagram of Cremophore EL-Capryol 90-Water system
Fig. 3
Fig. 3
In vitro dissolution profile of CMZ formulations (n = 3)
Fig. 4
Fig. 4
Chromatogram of the CMZ-MBG subjected to 40°C/75% RH at the end of 3 months
Fig. 5
Fig. 5
Chromatogram of forced degradation of CMZ in acidic conditions (1 N HCl)
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Lanchares JL, Hernandez ML. Recurrent vaginal candidiasis changes in etiopathogenical patterns. Int J Gynecol Obstet. 2000;71:S29–S35. doi: 10.1016/S0020-7292(00)00352-0. - DOI - PubMed
    1. Ferrer J. Vaginal candidosis: epidemiological and etiological factors. Int J Gynecol Obstet. 2000;71:S21–S27. doi: 10.1016/S0020-7292(00)00350-7. - DOI - PubMed
    1. Ritter W, Patzschke K, Krause U, Stettendorf S. Pharmacokinetic fundamentals of vaginal treatment with clotrimazole. Chemotherapy. 1982;28:37–42. doi: 10.1159/000238150. - DOI - PubMed
    1. Pavelic Z, Skalko-Basnet N, Jalsenjak I. Characterisation and in vitro evaluation of bioadhesive liposome gels for local therapy of vaginitis. Int J Pharm. 2005;301:140–148. doi: 10.1016/j.ijpharm.2005.05.022. - DOI - PubMed
    1. Pedersen M, Bjerregaard S, Jacobsen J, Sørensen AM. A genuine clotrimazole γ-cyclodextrin inclusion complex -isolation, antimycotic activity, toxicity and an unusual dissolution rate. Int J Pharm. 1998;176:121–131. doi: 10.1016/S0378-5173(98)00310-X. - DOI

Publication types

LinkOut - more resources