Estudo da Solubilização da Griseofulvina em Micelas dos Brijs 78, 98, 700

Abstract

The preparation of drug solutions with low solubility in water is one of the main problems found in the preparation of such medicines in aqueous medium. The study about the use of surfactant micellar solutions in the solubilisation of drugs with low solubility in water has been increasingly practiced, mainly due to the low toxicity of these carriers, to the efficiency of the dissolution process and to the additional protection provided to the drug. The objective of this work is to encapsulate the antifungic griseofulvin in poly(ethylene oxide) (Em) hydrophilic block copolymers and poly(methylene) (Cn) hydrophobic block. The copolymers (Brij® 700, Brij® 78, Brij® 98) and the griseofulvin were obtained from Aldrich. The Brijs critical micelle concentration (cmc) was reached through dye solubilisation method (fluorescence). The griseofulvin encapsulates were obtained through the method of direct dissolution and quantified by UV/Vis and 1H NMR and characterized by particle size through light scattering and X-Ray. The controlled release of the drug was carried out. The cmc values found for Brij® 78 and 98 are lower than those for Brij® 700. The size of the Brij® 700 particle, provided by the hydrodynamic radius (rh) is higher than those from Brijs® 78 e 98. The reason is that the hydrophilic portion of the Brij® 700 has 80 units more than Brijs® 78 e 98. The drug did not affect the size of the particle of the polymers. The solubilisation results for griseofulvin obtained through 1H NMR confirm the values obtained through UV/Vis. The griseofulvin had an increase in solubility up to 6.9 times, which makes the use of Brijs® feasible in the encapsulation of this drug.