Solubilização do fármaco Griseofulvina e da droga Oncocalixona A utilizando misturas dos copolímeros F127/P123/PEG35K como aditivo

Abstract

A continuing challenge of the health sciences and pharmaceutical industry is to improve the performance of drugs in the human body, reducing administration doses, toxicity levels and side effects, improving their efficiency. Thus, the objective of this work was to investigate the solubilization of the micellar solutions composed of the copolymer E98P67E98 (F127)/P123, as well as their mixtures, using the polymer PEG 35K as additive against the aromatic drug griseofulvin and the bioactive oncocalixone A, combining characteristics of gelification of F127 and solubilization. The methodology used in the solubilization of the drug griseofulvin was the direct dissolution method and, due to the fact that the bioactive oncocalixone A presented instability in this resource, it was studied through the solvent evaporation (Film) method. For the characterization of the copolymers and their mixtures the rheology was used and for the study of the gelling properties, the technique of tube inversion. In order to characterize the systems that presented the best solubilization results for oncocalixone A, infrared spectroscopy (FT-IR), rheology and in vitro release experiments were performed. Solubilization was measured by UV-Vis spectrophotometry and particle size by dynamic light scattering (Zetasizer). The copolymers P123 and F127 as well as their mixtures in the PEG 35K additive showed promising vehicles in the administration of the hydrophobic drug griseofulvin, the concentration of surfactant being 1% which provided the best solubilization result. The bioactive oncocalixone A presented a high solubility value, both in aqueous medium and in the presence of PEG 35K, when compared to the drug griseofulvin, the PF 50 mixture being in aqueous medium and in the presence of the additive, which proposed better values in the solubilization for this drug. It is seen from the particle size data in the presence and absence of the oncocalixone A drug that the mixtures as well as the compositions composed of the copolymers isolated in PEG 35K presented sizes below 200 nm, avoiding that there is a prior uptake and elimination by the phagocytic mononuclear system.