An overview of techniques for multifold enhancement in solubility of poorly soluble drugs

Abstract

Poor water solubility of newly discovered compounds has become the most common challenge in the drug development process. Indeed, poor solubility is considered as the root cause of failure of drug during drug development phases. Moreover, it has also been reported to be the main reason for bioavailability issues such as poor, inconsistent, incomplete and highly variable bioavailability of the marketed products. As per an estimate, approximately 90% of drug molecules suffer with poor water solubility at early stage and approximately 40% of the marketed drugs have bioavailability problems mainly due to poor water solubility. Solubility enhancement of the newly discovered compounds is primary research area for the pharmaceutical industries and research institutions. The conventional techniques to improve aqueous solubility of drugs employ salt formation, prodrug formation, co-crystallization, complexation, amorphous solid dispersion and use of co-solvent, surfactants or hydrotropic agents. Current advancement in the science and technology has enabled the use of relatively new techniques under the umbrella of nanotechnology. These include the development of nanocrystals, nanosuspensions, nanoemulsions, microemulsions, liposomes and nanoparticles to enhance the solubility. This review focuses on the conventional and current approaches of multifold enhancement in the solubility of poorly soluble marketed drugs, including newly discovered compounds.