Chapter 4 - Recent advancements in solubilization of hydrophobic drugs

Abstract

The improvement in the solubility of lipophilic drugs may play a vital role in the designing of products to attain not only high bioavailability but also therapeutic value at the site of interest. Importantly, nearly 40% of novel chemical moieties emerge with several hurdles at the time of screening in the pharmaceutical industry especially in the designing as well as in the formulation owing to their poor solubility in the aqueous phase, which also decreases bioavailability. Further, the drugs that come under Class II and Class IV in Biopharmaceutics Classification System (BCS) list those drugs which exhibit not only poor solubility in water but also reflect less poor dissolution rate and bioavailability. This chapter expounds different methods to improve solubility of drugs especially of hydrophobic nature, for instance, formation of complex with the drugs, solubilization by emulsification, solid dispersion methods, formation of salts, application of cosolvents, microemulsions/nanoemulsions, micronization of particles, crystal engineering, formation of micelles, and development of drug nanocrystals.