Optimization of Topical All-Trans Retinoic Acid Penetration Using Poly-DL-Lactide and Poly-DL-Lactide-Co-Glycolide Microparticles

摘要

All-trans retinoic acid has been, used in various therapies for treating acne, photoaging, psoriasis, keratinization disorders, acute promyelocytic leukemia, Kaposi's sarcoma, actinic keratoses and prevention and treatment of skin cancer. However, this drug promotes local irritation reactions that limit its topical use. Thus, the purpose of this study was to optimize retinoic acid therapy with the use of microparticles retinoic acid microparticles using PLA and PLGA were prepared and characterized. Skin penetration and skin irritation experiments were carried out. As results, PLGA microparticles presented high encapsulation efficiency (91%) and better release behavior than PLA microparticles.. In vitro retention studies showed that PLGA microparticles increased the retinoic acid concentration in viable skin when compared to the control (non-microencapsulated retinoic acid). As result of a skin irritation study in mice, it was observed that there was a significant reduction of irritation associated with retinoic acid topical therapy when PLGA microparticles were used. Therefore, PLGA microparticles containing all-trans retinoic acid may be a viable alternative for decreasing the skin irritation produced by the drug.