CARVEDILOL SOLUBILITY ENHANCEMENT BY INCLUSION COMPLEXATION AND SOLID DISPERSION: REVIEW

Abstract

Carvedilol is an antihypertensive drug characterized by itslow aqueous solubility, a major obstacle in drug formulation development to improve its bioavailability. To overcome problem of poor aqueous solubility of Carvedilol, various approaches have been investigated including physical and chemical modifications of the drug. Most of these investigations focused onmodifying the drug structurefrom crystalline insoluble form to amorphous soluble form, reducing drug particle size to provide high surface area subjected to solvent, enhancing porosity degree, and improving wettability. A wide variety of polymers was used in order to achieve these goals. Carvedilol inclusion complex with Cyclodextrin (CD) and derivatives, solid dispersion with water-soluble carriers such as Polyvinylpyrrolidone K-30 (PVP K-30), Gelucire 50/13, porous silica (Sylysia 350), and Soluprus® (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer) were previously investigated using different preparation methods such asSolvent evaporation method, fusion method, kneading method, and spray drying method. Analytical tests wereconducted to characterize these preparations. FTIR, SEM, DSC, XRD are among the most commonly used. The present paper summarizes different drug-carrier combinations used for solubility, dissolution rate and/or bioavailability enhancement of Carvedilol, with emphases on the preparation methods of Carvedilol inclusion complex and solid dispersions, and different tests used for their characterization. KEYWORDS: Carvedilol, solubility enhancement, inclusion complex, solid dispersion, bioavailability.