Development of nanostructured lipid formulation using myristyl myristate and ceramides in carrying of estradiol: physical-chemical e biological evaluation

Alopecia is a disease characterized by decreased or absent hair, which creates emotional stress for millions of men and women worldwide. The treatment of alopecia is carried out usually with topical application of drugs such as, sex hormone. However, this drug as well as others used in the treatment of alopecia have low efficacy. In this way the association of this drug with sustained delivery systems may increase the efficacy and reduce side effects. Thus, the aim of this work is the development and physico-chemical characterization of nanostructured lipid carriers (NLC) in the encapsulation of a steroid, aiming to increase the effectiveness of this drug in the treatment of alopecia. NLCs were prepared by the microemulsion of hot sonication method. The diameter and zeta potential were characterized , by using the technique of photon correlation spectroscopy and the average diameter obtained was 96 ± 15 nm while the average zeta potential was -16 ± 6mV. The encapsulation efficiency (EE) of the steroid measured by liquid chromatography with fluorescence detection was 99.6 ± 0.3%. In the study of physical stability of CLN stored at room temperature was observed that after two months the parameters diameter , zeta potential , pH , EE and recrystallization index (RI ) did not change significantly , demonstrating that this project has developed CLN great potential as a delivery system of 17-alpha- estradiol. The power dermal penetration of CLN was evaluated in Franz diffusion cell and confocal microscopy, and the results indicate that there is accumulation of CLN in the outer portions of the epidermis, especially the hair follicle, suggesting that this formulation is within the standards of biosecurity. Furthermore, evaluations of internalization of CLN on keratinocytes cells demonstrated that nanocarriers were internalized and accumulated mainly in the cytoplasm (AU)