Non-Aqueous Phospholipid Concentrates for Increasing the Bioavailability of Poorly Soluble Compounds

Abstract

The properties and use of liquid non-aqueous phospholipid concentrates (NAPC) are reviewed. They are mainly used to solubilize poorly water-soluble drug substances to enhance their oral bioavailability, but they also find applicability in dietetics and cosmetics. Due to the large-scale availability of these concentrates at good manufacturing practice quality including Drug Master File (DMF) documentation, they can be used for pre-clinical screening and clinical testing and as market form, as demonstrated by the product of Wyeth/Pfizer, Rapamune, enabling a cost effective and fast dosage form development. When needed, NAPC can be converted to solid dosage forms by means of a capsule fill or addition of adsorbing excipients. It is concluded that NAPC deserve more attention and a broader use in the life science industry. Practical Applications: NAPCs are suitable as pre-clinical formulation vehicle for screening of the oral bioavailability of poorly water-soluble compounds. The same formulation can be used for clinical testing and market introduction, allowing a fast track dosage form development. When needed NAPC can be converted to solid dosage forms. NAPC have also applicability in dietetics and cosmetics to solubilize poorly water-soluble compounds.