Development of polymeric microneedles for topical treatment of melasma

Abstract

Melasma is a common acquired hyperpigmentation disorder that mainly affects women during their childbearing and reproductive years. It is characterized by irregular light to dark brown spots on the face, which negatively impacts the patients well-being and quality of life. Although its pathogenesis remains unclear, several etiological factors have already been identified as risk factors for the development of melasma, including exposure to sunlight and visible light, genetic predisposition, pregnancy and use of exogenous hormone (combined contraceptives and hormone replacement therapy). Although its global prevalence is still unknown, it is estimated that 9-50% of the population exposed to the risk factors have melasma. In addition, 8-34% of women who use exogenous hormone and 10-70% of pregnant women, develop melasma in the world. Specifically in Brazil, the disease affects around 15-35% of adult women. Unfortunately, among all the treatments currently available to treatment of melasma, most of them produce inconsistent and generally unsatisfactory results, in addition to being mostly irritating and aggressive to the skin. Therefore, given the negative impact of melasma on quality of life and the clinical and therapeutic challenges associated with it, the search for a more effective alternative with a sustained and long-term effect for patients with this frustrating and therapeutically challenging disorder has been one of the main focus of the global Pigmentation Disorders Treatment (TDP) market, which has grown steadily in recent years (CAGR of 6.75% between 2017-2025). In this context, the main of this Phase I PIPE Project is to develop polymeric microneedles (MAPs) for sustained, minimally invasive and painless release of active ingredients with proven anti-melanogenic effect on the skin, overcoming the limitations of conventional therapies. This Phase I study will consist in two stages: Stage I: R&D of different systems with MAPs, and evaluation of the mechanical properties and penetration efficiency in artificial membrane; Stage II: in vitro and ex vivo evaluation of the drug release and skin penetration profile in pig ear skin. It is expected to obtain MAP with potential for safe and effective topical treatment of melasma. (AU)