Abstract

Objective: The objective of the present work was to develop, characterize and evaluate the tioconazole loaded emulgel and to prove that emulgel can be the best alternative for delivery of hydrophobic drug topically.Methods: for the preparation of stable Emulgel, firstly gels were prepared using different polymers as carbopol 934 and xanthan gum, followed by preparation of emulsions and finally mixed together (table 1). Emulgel was evaluated for physical appearance, pH, spreadability, extrudability, viscosity, swelling index, dilution test, centrifuge test, drug content, in vitro release study, kinetic analysis of release data, antifungal activity and stability study for 3 mo. A comparative study was also performed between prepared emulgels with available marketed antifungal cream.Results: All evaluation parameters were in acceptable range with good physical appearance and the pH in the range of 5.5 to 6.8. The results show that the extrudability was in the range 15.63 to 35.27 g/cm2; with spreadability in range of 6.6 to 8.833 cm. swelling index of F3 was seen a maximum in 3 h of about 75.13%. The viscosity was in the range of 15240 to 56340 cps at 10 RPM. During in vitro release of all formulations, F1 and F5 showed a maximum in vitro drug release of 59.11% and 55.11% respectively in 8 h. The kinetic analysis of fitting the data in different model shows that the best formulation of F1 fits in the Higuchi model with regression coefficient (R2) of 0.998 and show non-fickian diffusion. The formulations were found stable. F1 and F5 provide a similar zone of inhibition like to market cream.Conclusion: Tioconazole emulgel provide the better platform for delivery of hydrophobic drug for topical route and so able to produce better patient compliance.

Highlights

  • Topical drug delivery is the potential route to deliver the drug producing low side effect in comparison with any other dosage forms

  • Tioconazole has considerably greater fungicidal activity than clotrimazole, econazole, ketoconazole, and miconazole against Candida albicans and other Candida species. tioconazole is highly hydrophobic in nature that lies in Biopharmaceutical classification system (BCS)-II class [4, 5]

  • Tioconazole Emulgel was formulated and compared with marketed cream and proved that emulgel can be, the better option than conventional as it minimizes the disadvantages associated with conventional semi-solid increasing the patient compatibility

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Summary

Introduction

Topical drug delivery is the potential route to deliver the drug producing low side effect in comparison with any other dosage forms. The new approach in the field of topical drug delivery is introduced to deliver the hydrophobic drug that can enjoy the gelling property and whose rate can be controlled named Emulgel. It is where emulsion of the drug is prepared and that are incorporated in the gel [3]. Tioconazole is an antifungal agent of imidazole class which is used to treat infections caused by a fungus or yeast. Tioconazole has considerably greater fungicidal activity than clotrimazole, econazole, ketoconazole, and miconazole against Candida albicans and other Candida species. tioconazole is highly hydrophobic in nature that lies in Biopharmaceutical classification system (BCS)-II class [4, 5]

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