Desenvolvimento e aplicação de carreadores lipídicos nanoestruturados contendo finasterida para o tratamento de alopecia androgenética

Abstract

Beyond its aesthetic importance, hair distinguishes the individual and can influence social acceptance. Under certain circumstances, the normal hair growth process is impaired by a very common physiological disorder called androgenetic alopecia (AGA). The hair loss is the consequence of an increased expression of 5α-reductase enzyme that converts testosterone into dihydrotestosterone. To treat AGA, finasteride, an antiandrogenic steroid, can be used in two forms: oral or topical. However, for both forms, side effects such as irritation, decreased libido, contact dermatitis and mood changes have been reported. The use of nanocarriers as a vehicle for drugs can reduce such side effects by reducing the need for high doses or concentrations and frequent reapplications. The objective of this study is to develop nanostructured lipid nanoparticles containing finasteride (NLC-FNS07) for androgenetic alopecia treatment. As a preview result, it’s showed here the construction of the nanoparticles with natural origin lipids adjusted to release on defined temperature and stabilized with copolimers in block. Such nanoparticles were built with natural origin lipids adjusted to release the drug in specific temperature and stabilized with block copolymers. After preparation using ultrasonic irradiation, the lipid nanocarriers produced exhibited hydrodynamic diameter with average size of 119.56 ± 1.07 nm and polydispersity index of 0.186. Due to the hydrophobic characteristics of the drug, the encapsulation efficiency reached values close to 100% after HPLC quantification. The suspension kept its characteristics through 30 days, showing good stability. In addition, the nanostructures reduced the finasteride cytotoxicity for fibroblasts and keratinocytes cells. Subsequently, permeation, controlled release and in vivo efficiency tests were carried out. NLC-FNS07 improved the drug stability and skin permeation, while reducing skin irritation and inflammation, without systemic absorption. Finally, it showed efficient hair restoration in vivo, and remained in the epidermis, including the bulbs, suggesting safety for topical administration. The promising efficacy of our novel NLC-FNS07 in AGA treatment designates it as a good candidate for therapeutic applications.