Fluorescence emission applied on the evaluation of antiparasitic micellar systems. Elucidation of the molecular mechanism of the solubilisation process.

PRIOTTI, J.; LAMAS, M. C.; PICO, G.; LEONARDI, D.

AAPS PHARMSCITECH

SPRINGER

Lugar: Berlin; Año: 2017

1530-9932

Poor aqueous solubility represents a major challenge in achieving adequate oral bioavailability for drug development nowadays. Albendazole and ricobendazole have been listed as class II compounds in the Biopharmaceutical Classification System, being the poor solubility a significant issue to modify and to improve. The main goal to formulate oral dosage forms is to get the molecular state of the drug by solubilization in the gastric fluid. Micellar systems are excellent pharmaceutical tools to perform the proper solubilization and absorption of poorly soluble compounds. In this study, physicochemical properties of micellar solutions of albendazole and ricobendazole were thoroughly investigated. Two biosurfactants have been selected, sodium cholate and sodium deoxycholate, and two synthetic flexible chain polymeric surfactants, poloxamer 407 and polisorbate 80, to study the solubilization process of the poorly soluble anti-parasitic agents. Fluorescence emission was applied to obtain surfactant/drug stoichiometry ratios, critical micellar concentration, protection efficiency of surfactant micelles and thermodynamic parameters. In addition, micellar systems were characterized by their size and zeta potential, considering the pH effect.