Novel microemulsion-based gel formulation of tazarotene for therapy of acne

Abstract

The objective of this study was to develop and evaluate a novel microemulsion based gel formulation containing tazarotene for targeted topical therapy of acne. Psudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, and co-surfactant for microemulsion formation. The optimized microemulsion formulation containing 0.05% tazarotene was formulated by spontaneous microemulsification method consisting of 10% Labrafac CC, mixed emulsifiers 15% Labrasol–Cremophor–RH 40 (1:1), 15% Capmul MCM, and 60% distilled water (w/w) as an external phase. All plain and tazarotene-loaded microemulsions were clear and showed physicochemical parameters for desired topical delivery and stability. The permeation profiles of tazarotene through rat skin from optimized microemulsion formulation followed the Higuchi model for controlled permeation. Microemulsion-based gel was prepared by incorporating Carbopol®971P NF in optimized microemulsion formulation having suitable skin permeation rate and skin uptake. Microemulsion-based gel showed desired physicochemical parameters and demonstrated advantage over marketed formulation in improving the skin tolerability of tazarotene indicating its potential in improving its topical delivery. The developed microemulsion-based gel may be a potential drug delivery vehicle for targeted topical delivery of tazarotene in the treatment of acne.

• Acne
• microemulsion
• skin irritation study
• skin retention study
• tazarotene
• topical drug delivery

Acknowledgements

The authors are thankful to Astron Research Ltd (Ahmedabad, India) for the gift sample of TZR pure powder, Sophisticated Instrumentation Center for Applied Research, and Testing (SICART) (Vallabh Vidyanagar, India) for providing facilities for carrying out analytical work, Gattefosse (Saint-Priest, France), Colorcon (Asia) Pvt. Ltd. (Mumbai, India), Abitec Corporation (Janesville, WI), BASF (Mumbai, India), Sasol (Witten, Germany), Lubrizol Advance Material India Pvt. Ltd. (Mumbai, India), Noveon (Cleveland, OH) for providing samples of excipients; to Dr. A. M. Thakar, Dr. Zala, Dr. Kalyani, and Dr. Mathakiya, Veterinary Science College, Anand Agriculture University, Anand for providing guidance and research assistance for skin irritation study, and Dr. Venu Mehta, Department of Humanities and Social Sciences, CHARUSAT, Changa, Anand for checking the manuscript.

Declaration of interest

The author(s) confirm that this article content has no conflicts of interest.