Establishment of Preparation and Evaluation Methods of Drug Amorphous Nanoparticles to Dramatically Improve Drug Solubility and Absorption

Abstract

Amorphous nanoparticle composed of poorly water soluble glibenclamide (GLB) and stabilizer hypromellose (HPMC) was prepared by two antisolvent methods. In method A, DMSO solution containing GLB was poured into water containing HPMC to prepare nano-A suspension. In method B, a DMSO solution containing both GLB and HPMC was poured into water to obtain nano-B suspension. The morphology of nano-A and nano-B was spherical hollow and deformed non-hollow particles, respectively. The GLB amorphous was more stable in nano-A than in nano-B during heating process, because GLB and HPMC in nano-B was more miscible than in nano-A. The stability of the amorphous GLB in nanoparticles was strongly affected by GLB/HPMC miscibility, depending on their methods of preparation.

Graphical Abstract

Schematic representation of precipitation process and structure of (a) nano-A and (b) nano-B.