Role of Coformers in Solubility Enhancement of Poorly Soluble Drugs through Cocrystallization: An Overview

Abstract

Improving the solubility of poorly soluble pharmaceuticals is a key problem in the pharmaceutical industry, and it can be solved using a range of methods, such as particle size reduction, surface modification, and other procedures. Cocrystallization is a new method for enhancing solubility in the pharmaceutical industry, which can be done with the help of cocrystal former (Coformer). These are water- soluble stoichiometric cocrystals of the active pharmaceutical ingredient (API) with water-soluble small molecule coformers such as ascorbic acid, Nicotinamide etc. Selection of coformer is a principal challenge in evolution of cocrystals, which can be done by various approaches such as trial and error, supra molecular synthon, virtual screening, etc. Hydrogen bonding, halogen bonding, and π-π interactions all play a part in the development of cocrystals. Moisture absorption, cocrystal reactant dissolution, cocrystal nucleation, and growth are all factors that impact crystal formation. Cocrystals can be prepared by various methods such as Solution evaporation method, Solution cooling crystallization, Solid state grinding, Liquid assisted grinding method, Hot melt extrusion, etc. This review complies the various research works on cocrystals.