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

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.