Amorphous Dispersions and Other Tools for Drug Discovery Formulation Support

March 31, 2013


Bloom, C.J., and D.K. Lyon, “Amorphous Dispersions and Other Tools for Drug Discovery Formulation Support,” Drug Dev. Delivery, 13:3(2013)32-37.


Low-solubility compounds are commonly encountered in the drug discovery process. It is widely estimated that more than half of the promising small molecules identified in current drug discovery programs exhibit low solubility. Molecules with low permeability and rapid metabolism also plague discovery programs. Each of these shortcomings poses challenges for oral absorption, which must be addressed because of the prevalence of new compounds that fall into these categories.

This paper describes broadly applicable formulation approaches and biomodeling tools that have been successfully used to improve the solubility and in vivo performance of low-solubility compounds. The approaches, including spray-dried drug/polymer dispersions and drug/polymer nanoparticles, are ideally suited for use early in the drug development process from discovery through formulation and toxicology screening. In addition, the approaches are readily scalable, facilitating progression of compounds through commercial manufacture. Combined with the judicious use of biomodeling tools, these approaches can result in efficient selection of compounds and formulations for advancement.



Bioavailability Enhancement