Formulation of poorly water-soluble drugs via coacervation - A pilot study using febantel

In this study, febantel was dissolved under increased temperature in a nonionic surfactant Lutrol L44 (R) and subsequently mixed into an aqueous maltodextrin solution. After 8 h under static conditions, coacervation or phase separation took place. H-1 NMR spectra and HPLC analysis showed that the upper phase contained mainly all febantel, while no febantel was detected in the lower phase. Fluorescent microscopy showed that maltodextrin is distributed in the lower phase. Coacervation proved to be a promising formulation technology for certain poorly water-soluble drugs, such as febantel. The coacervate phase showed an increase in in vitro dissolution kinetics, compared to Rintal (R) granules. These results were confirmed in an in vivo study performed on dogs. Febantel and fenbendazole showed a significant increase in plasma concentration compared to Rintal (R) granules. Further studies have to be performed to transform coacervates into a solid dosage form and to prove broad applicability to other poorly soluble drugs. (C) 2013 Elsevier B.V. All rights reserved.