Abstract: Compositions and procedures that yield sub-micron and micron-size stable particles of water-insoluble or poorly soluble drugs or other industrially useful insoluble compounds are prepared using combinations of natural or synthetic phospholipids, a charged surface modifier such as a highly purified charged phospholipid and a block copolymer coated or adhered onto the surfaces of the water insoluble-compound particles. The combination of charged surface modifier and block copolymer allows the formation and stabilization of the sub-micron and micron size compound particles—stabilized by the charged phospholipid to provide electrostatic stabilization and the block copolymer to provide steric stabilization—and therefore prevents these particles from particle growth, aggregation or flocculation.

Abstract: Pharmaceutical compositions comprising electrostatic and steric-stabilized sub-micron and micron-size stable microparticles of water-insoluble or poorly soluble drugs or other industrially useful insoluble compounds having diameters of about 0.05 to about 10 microns are described. The particles have phospholipid coated surfaces and are stabilized with a combination of charged surface modifier and block copolymer. The diameter of the particles is greater than about 50% but less than 100% of the diameter of particles comprising the poorly soluble drug and the phospholipid coated surfaces prepared by otherwise identical means in the absence of the combination of charged surface modifier and block copolymer. The charged surface modifier provides electrostatic stabilization and the block copolymer provides steric stabilization that minimize particle size growth caused by Ostwald ripening and particle aggregation and provides for small particle formation.