Development of Nanocrystals of Poorly Water Soluble Drugs For Improved Delivery

Abstract

Poor water solubility is the main problem in developing various pharmaceuticals. Nowadays, to improve the solubility of various formulations, specific strategies are being involved for their dissolution and bioavailability. The objective of the present work was to improve the solubility of low water-soluble aceclofenac and ziprasidone by preparing stable nanocrystals of the drugs. Nanocrystals of aceclofenac and ziprasidone were prepared by the combination of precipitation processes using antisolvent technique, high pressure homogenization and wet media milling technique required for stabilization and conversion into fine and dry crystals using spray-drying. The drugs and their nanocrystals were characterized by SEM, FTIR, XRD, as well as by measuring their particle size. The XRD results indicated that the antisolvent precipitation with high-pressure homogenization led to the crystallization of aceclofenac and wet media milling led to the crystallization of ziprasidone. The nanocrystals, thus produced, led to the stabilization of drugs by adsorption of the stabilizers onto the drug surfaces. Nanocrystalllization increased the solubility of both the drugs by almost fourfold. The combination of the two methods for forming nanocrystals led to the formation of a stable formulation, which showed increase in solubility by increment in effective surface area and amorphous nature of the drugs. newline newline