Drug Loading and Dissolution Properties of Dalcetrapib-Montmorillonite Nanocomposite Microparticles

This work aims to transfer the fast dissolution performances of drug nanosuspensions into the solid state via a carrier particle-mediated isolation method and explores the factors affecting the maximum achievable drug loading of the prepared nanocomposite microparticles. The solid composites of fast dissolving dalcetrapib (DCP) nanoparticles on larger montmorillonite (MMT) carrier microparticles have been prepared by an antisolvent precipitation method. The very high dissolution rate of the DCP nanoparticles is combined with the simple solid-liquid separation and drying of the MMT composite microparticles. The fast dissolution rate of DCP from the solid-state nanocomposite microparticles was maintained up to a drug loading of 20.9%, and the formulation was stable for a minimum of 10 weeks in the solid state. Surface functionalization of the MMT particles was not needed for a high and uniform attachment of nanoparticles. Addition of soluble surfactant and polymeric additives, generally used for stabilization of nanosuspensions, was not required and even decreased the DCP nanoparticle attachment and thus limited drug loading.