Development of solid lipid formulation using nanostructured Myristyl Myristate and ceramides in carrying of estradiol: physico-chemical and biological evaluation

Abstract

Alopecia is a disease that affects 50% of men at age around 50 and almost to a 50% of women. This disease is characterized by decreased or absent of hair, which creates emotional distress for millions of men and women in the world. The treatment of alopecia is performed, in general, for topical application of drugs, for example, by 17-alpha-estradiol which is a stereoisomer of the sex hormone 17 - beta-estradiol. However, this drug, as well as others used in this treatment, has a low efficacy. In this line the combination of the drug with sustained delivery systems, such as solid lipid nanoparticles, can increase the efficacy and reduce side effects.Thus, the main of this work is the development and physico-chemical and biological characterization solid lipid nanoparticles using butter Theobroma grandiflorum (cupuaçu) in the encapsulation of 17-alpha-estradiol to increase the effectiveness of this drug in the treatment of alopecia. The solid lipid nanoparticles are prepared by the method of high pressure homogenization, and it will be characterized the morphology by atomic force microscopy (AFM), and the diameter and zeta potential using the technique of photon correlation spectroscopy. The encapsulation efficiency and kinetics of release of estradiol will be analyzed by liquid chromatography / mass spectrometry. The power of transcutaneous penetration of the particles will be measured in Franz diffusion cell. In addition, toxicity assessments will be performed in vitro in cell keratinocytes. It is expected that the solid lipid nanoparticles increase stability and skin permeation of estradiol, thereby potentiating the effects and allows to use lower dosages and reducing the side effects.