Microwave generated nanocomposites for making insoluble drugs soluble

In order for a drug to be bioavailable the human body must absorb it, and in oral treatments absorption takes place, after drug dissolution, by diffusion of the molecules through the gastrointestinal (GI) membranes. Since the GI tract is an aqueous environment and more than one third of the existing drugs are poorly soluble or insoluble in water, solubilization of water-insoluble drugs is a big issue of pharmaceutical research. The key-concept of solubilization is to force the insoluble solid to assume a (metastable) microstructure characterized by nanoscale periodicity. Our research, starting from this scene, is based on the following facts: (a) the most advanced approaches to water-insoluble drugs solubilization are based on generating a drug dispersion (at molecular and/or nanoscale level) in a stabilizing media, preferably in solid-state form, (b) the polarizing aspect of microwave (MW) heating produces several specific excess effects, in particular enhanced mass transport, thus providing a green, effective tool for generating drug solid dispersions, and (c) with few exceptions pharmaceutical (organic) materials are diamagnetic and dielectric, i.e. are suitable for MW heating. We developed a method based on MW induced diffusion (MIND) for generating activated drug/3D-matrix nanocomposites. This innovative (and environmentally friendly) solid-state solubilization technique will be presented and discussed. (C) 2003 Elsevier B.V. All rights reserved.