Poor aqueous solubility-an industry wide problem in drug discovery

By C. Lipinski. 2002

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Drug Nanoparticles: Formulating Poorly Water-Soluble Compounds (2008, background): “THE SOLUBILITY CHALLENGE It is estimated that ~40% of active substances identified through combinatorial screening programs are difficult to formulate as a result of their lack of significant solubility in water (Lipper, 1999; Lipinski, 2000, 2002).”
Nanosuspensions: a promising drug delivery strategy (2004, background): “…of poorly water-soluble drugs has always been a challenging problem faced by pharmaceutical scientists and it is expected to increase because approximately 40% or more of the new chemical entities being generated through drug discovery programmes are poorly water-soluble (Lipinski 2002).”
Nanoparticle technology for drug delivery (2006, background): “The increased surface area of nanoparticles can significantly increase the dissolution of poorly water-soluble drugs, which are estimated to comprise 40% of drugs under development (Lipinski, 2001, 2002).”
Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products. (2008, background): “…databases were queried on 29/03/2008 Given the increasing number of compounds emerging from discovery programs having poor solubility and/or dissolution rate (Lipinski, 2002), pharmaceutical scientists are constantly seeking new formulation approaches in order to obtain adequate oral…”