Design and development of tranexamic acid loaded film‐forming gel to alleviate melasma

Abstract

Background Melasma is a skin condition that causes increased epidermal pigmentation, enlarged melanocytes, increased melanosomes, solar elastosis, dermal blood vessels, and, occasionally, perivascular lymph histiocytic infiltrates. Objective To develop the film‐forming gel to alleviate melasma. Tranexamic acid was used as a model drug to evaluate the suitability of formulation to prevent symmetric hyperpigmentation. Methods FFG is a hydrophilic polymeric cross‐linked system loaded with an active moiety. Nine different formulations of 2% TXA were formulated using polyvinyl alcohol and hydroxypropyl methylcellulose 50 cP as film‐forming polymers. Sodium carboxymethylcellulose, methylcellulose, and carbopol were used as gelling agents. Results F7, F8, and F9 showed shorter DT, that is, 11, 8, and 12 min, respectively. The folding endurance of F7, F8, and F9 was >100 folds, and the pH of F7, F8, and F9 was >6. Among three formulations, F8 was further analyzed for in vitro drug diffusion, which showed >95% drug diffusion within 48 h. In vivo, the skin irritation potential of F8 was estimated using BAL/C mice, which confirmed the absence of skin irritation. Conclusion From the obtained results, we conclude that the FFG can be a strategic attempt to deliver the cosmeceutical drugs like TXA to alleviate Melasma with improved sustainability of the drug.