Otimização de Formulações Micelares do Pluronics ® F127 para Solubilização e Liberação de Bioativos.

Abstract

The drug delivery systems is a topic that has received much attention in the last decades in the pharmaceutical sector, due to the large therapeutic benefits and the economic advantages. The study on the use of copolymers in the dissolution of poorly water soluble bioactive has been increasingly practiced, mainly due to the low toxicity of these carriers and their high efficiency in the process of dissolution. Using polymer surfactants forming micelles in solution, it is possible to increase the solubility and act in the controlled release of hydrophobic bioactive in the body. This study aimed to investigate the use of the polyethylene glycol (PEG) polymer as an additive in aqueous solutions of Pluronic® F127 copolymer, developing solubilization studies, release and cytotoxicity in human neutrophils with the aim of optimizing the solubilization of bioactive griseofulvin, quercetin and mangiferin. Using the tube inversion technique to study the gelling properties of mixtures of F127 and PEG 400, 6K and 35K. The system containing the polymeric additive PEG 400, 6K and 35K are shown as promising alternatives for use in subcutaneous administration of hydrophobic bioactive, being compatible with the gelling characteristics of F127 pure constituents as promotes a decrease in concentration of formation gel. For the three bioactive study, it was observed that the micellar structures F127 immersed in 1% PEG 6K additive at a concentration of 0.5% showed good solubility values as compared to other percentages, the bioactive was quantified by UV-Vis spectroscopy. The cytotoxicity was investigated by LDH activity in human neutrophils (5 x 106 cells / ml). In general, the systems (PEG 6K 0.5% + 1% F127) have show no significant cytotoxicity.