OBTENÇÃO, CARACTERIZAÇÃO FÍSICO-QUÍMICA E AVALIAÇÃO BIOLÓGICA DE NANOPARTÍCULAS DE BLENDAS DE PLA-PEG CONTENDO ÁLCOOL PERÍLICO

Abstract

Perillyl alcohol (POH) is a monoterpene coming from of limonene, found in essential oils of many plants and citrus fruits, and is being increasingly studied by presenting promising activity against several tumors, such as breast, lung, gliomas, among others. Spite of presenting excellent clinical results, the POH presents some drawbacks: necessity of multiple doses during the day and the side effects, mainly related to the gastrointestinal tract. This study aimed to the development of polymeric nanoparticles, with the intention of providing a controlled release that can reduce the toxicity and the need for multiple doses. The mobile phase was composed of ACN: water (80:20 v / v), with a flow 1mL/min and with detection at 210nm. The method developed showed all the necessary parameters according to current recommendations. The percentage of encapsulation efficiency of nanoparticles was 54,61%, with a size of 229,46 nm, with a homogeneous size distribution and spherical shape. Zeta potential was obtained of -21 mV. The physicochemical analyzes (x-ray, infrared spectrophotometer and differential scanning calorimetry) showed that the process of nanoencapsulation formed an amorphous system. With the stability study it was determined that better of nanoparticles storage condition is under refrigeration (8 ° C), in which nanoparticles remained stable at study period of three months. POH nanoparticles released approximately 30% at 168 h, with the release kinect profile determined as second order with a release performed through the diffusion the POH. In the cytotoxicity test against the erythrocytes, both unencapsulated POH as the nanoparticles blends of PLA - PEG containing POH not showed cytotoxic effects against this tested model. HEp-2 cells showed 60% cell viability in the presence of POH nanoparticles, in 96 hours. With the tests conducted it was concluded that the nanostructured system containing POH was successfully obtained, which has a potential for application in treatments against tumors.