COMPLEJOS NANOPARTICULADOS INTERPOLIELECTROLITO-FÁRMACO COMO PORTADORES DE FÁRMACOS BÁSICOS

PALENA, MARÍA CELESTE; ALLEMANDI, DANIEL; MANZO, RUBÉN HILARIO; JIMENEZ KAIRUZ, ALVARO FEDERICO

Tandil, Agentina

Congreso; 40° Reunión Anual de SAFE; 2008

Sociedad Argentina de Farmacología Experimental

The aim of this project was the obtention of polyelectrolyte/drug complex nanoparticles (NP). With this purpose two polymetacrilates, one anionic (eudragit L100 (EuL) and other cationic (eudragit E100 (EuE)) were selected to prepare ionic complexes with the model drugs (D), atenolol and propranolol. Aqueous dispersions of the obtained particles were subjected to physicochemical characterization and in vitro release studies. Aqueous dispersion of EuL were neutralized with D, then different proportions of EuE were added to obtain (EuL-D₅₀-EuE_x) complexes (the subscript indicate the mole% of EuL-carboxylic groups neutralized with D or EuE, x=25, 50, 75, 100%). NP were characterized through ultracentrifugation, optical density, Z-potential, light scattering, microscopy and pH determinations. In vitro release was performed in Franz cells with synthetic membranes and water or physiological soln. as receptor media. The capacity of NP to be loaded with D increases from 57 to 80 w% with increase in the proportion of EuE but their physical stability decreases. D release from NP is slow when water is the receptor medium but it rises when physiological soln. is used. The rate and anomalous-kinetic remain unchanged with EuE and D proportions are modified. At present, permeability essay in everted rat intestine are being performed. This system of NP has potential properties to be used as D controlled release carriers.