Desenvolvimento e avaliação de nanopartículas lipídicas sólidas contendo papaína em modelos in vitro de leishmaniose cutânea

Abstract

Cutaneous Leishmaniasis is the most common form of leishmaniasis. Nowadays, the treatments available for this disease are toxic, long and expensive. Therefore, the search for new molecules with antileishmania potential is emphasized. In this scenario, papain is a proteolytic enzyme with medicinal properties, such as anti-inflammatory, healing and anti-parasitic. However, it is a protein that has limitations in terms of its application, such as low stability and high sensitivity. Hence, the development of methodologies for immobilizing enzymes appears as a powerful strategy. In special, nanotechnology presented advantages due to the incorporating and transport of drugs and biomolecules, in addition to improving stability, ability to cross biological barriers and proceed to the targeted action site. The aim of the present study is to obtain solid lipid nanoparticles (SLNs) based on 1,3-distearyl-2-oleyl glycerol (TG1) triglyceride and to monitor the physicochemical properties for modified papain release. The solid lipid nanoparticles were produced by the emulsification method with solvent evaporation and the incorporation of papain by the adsorption method (SLNPAP). The physical-chemical characterization of the nanoparticles, demonstrated that the NLSs had a diameter smaller than 300 nm, with uniform particle size distribution and zeta potential of -13.2 ± 0.26 mV. SLNPAPs presented larger particle size and a less negative zeta potential (-2.08 ± 0.22), corroborating with the infrared spectroscopy (FTIR-ATR) data. The formulations showed, for morphology, spherical shape and smooth surface, observed by the techniques of atomic force microscopy (MFA), scanning electron microscopy (SEM). NLSTG1 and NLSPAP formulations were biocompatible in assay with NIH3T3 and Vero E6 cells. The SLNTG1 and SLNPAP formulations were biocompatible and increased the papain antileishmania activity by 20%. Therefore, the present study, systematically addresses the nanocarrier development with innovative capacity to incorporate papain and increase the effectiveness of its possible application in antileshmania activity.