Evaluation of skin permeability characteristic of tranexamic acid with different formulation approaches

ABSTRACT The aim of this study was to develop a topical Tranexamic acid (TXA) gel (10%) for treating skin pigmentation with targeted delivery, enhanced permeation, potential cost-effectiveness, and ease of use. This formulation warrants further investigation for efficacy and safety in managing pigmentation. It was developed many topical formulations using (TXA) for the purpose of treating skin pigmentation. The objective was to develop a user-friendly therapy with low adverse reactions and great efficacy. The primary objective was to enhance the skin penetration capability of TXA. It was tested nine different hydrogel mixtures and found that one with 3% hydroxypropyl methyl cellulose ( HPMC) released the most TXA over the course of five hours of in vitro testing. However, subsequent experimentation on pig skin (ex vivo) revealed that this compound did not sufficiently permeate the skin. This is likely due to the water solubility of TXA, which hinders its ability to penetrate the epidermal barrier. To overcome this constraint, it was investigated two approaches to improve TXA penetration: Microneedling is a procedure that involves using a tiny roller equipped with needles to create temporary channels in the skin. During experiments, microneedling demonstrated a substantial increase in the quantity of TXA released from the HPMC formulation. In another approach, it was designed a formulation approach that encased TXA in tiny particles made of lecithin, a lipid compound. In ex vivo experiments, the nano sized lecithin hydrogel formulation demonstrated potential by exhibiting a continuous release of TXA for a duration of 24 hours. This can be due to the synergistic effect of lecithin's characteristics and the diminutive particle size may account for this technique's superior efficacy. Both microneedling and nano sized-lecithin hydrogels work well to improve the penetration of topical TXA therapies into the skin to manage pigmentation problems. Further investigation is required to design a medication that is both secure and efficacious for this ailment. Keywords: Topical TXA formulation, Skin pigmentation, HPMC hydrogel, Microneedling, nanosized lecithin hydrogel, ex vivo permeation