Obtenção de nanopartículas poliméricas a base da goma do Cajueiro acetilada para incorporação de epiisopiloturina

Abstract

Natural products are taking an increasing interest in the current situation due to its potential application in a wide variety of traditional and emerging sectors, such as the production of biocompatible materials for biomedical devices. Thus, we emphasize the use of natural polymers that have favorable characteristics for biomedical and pharmaceutical applications,

among which we highlight abundance, renewal, biodegradability, biocompatibility, non- toxicity, besides being inexpensive sources. The cashew gum is a polysaccharide extracted from

Anacardium occidentale L. species, a tropical plant extensively cultivated in northeastern

Brazil. Biomedical gum cashew stands out for its gastroprotective effect, anti-diarrheal, anti- tumor, modulatory macrophages, effective in the topical treatment of wounds. As well, there is

still the use of derivatives in the production of polymeric nanoparticles for incorporation of drugs, which enables a controlled and sustained release. The epiisopiloturine (EPP), also a natural product extracted from the leaf Jaborandi is an imidazole alkaloid, which has a proven activity in vitro against Schistosoma mansoni and in a more recent study has shown promising anti-inflammatory and analgesic effect. In this context, it sought to nanoformulate EPP in a polymer system of acetylated cashew gum to allow a controlled release, thus increasing the therapeutic benefit while minimizing possible side effects. The nanoparticles were synthesized by dialysis technique, two polymer concentrations and different proportions polymer: alkaloid. The average size and polydispersity index (PDI) were determined by dynamic light scattering analysis (photon correlation spectroscopy - DLS) and zeta potential was determined from the electrophoretic mobility of the samples. It was determined the amount of EPP incorporated in the nanoparticles, and they were analyzed by Atomic Force Microscopy (AFM) and Nanoparticle Tracking Analysis (NTA). To understand the in vitro release mechanism the data were treated by Korsmeyer-Peppas method. The synthesized nanoparticles have average sizes between 108.6 and 154.4 nm and PDI between 0.120 and 0.212. The zeta potential was negative for all formulations with and without active. An encapsulation efficiency was identified of up to 55% of epiisopiloturine. The analysis of images obtained by atomic force microscopy to suggest that the nanoparticles have spherical shape and are distributed in an aggregated manner. The size of the nanoparticles by NTA are in line with those obtained by DLS. Furthermore, the nanoparticle concentration is between (92.4) x 109 and (136.5) x 109 particles/mL. The release of nanoformuled epiisopiloturine occurred slowly and gradually, presenting a balance by around 6pm release. The value of n was found to be 0.37 for the release of EPP, it is possible to say that the mass transfer follows the Fickian diffusion model. The results showed that the acetylated cashew gum nanoparticles incorporated with EPP have nonometric colloidal systems characteristics and allowing a slow and gradual release profile, with Fickian diffusion type thus making it feasible ways of nanoparticle formulations.