Journal of Bioequivalence & Bioavailability

Enhance oral bioavailability of hydrophobic compounds by using polymeric nanoparticles

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Ying Liu, Magdalena Szymusiak and Hao Shen

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

Nearly 40% of all pharmaceutical compounds on the market and 90% of newly developed compounds are hydrophobic, and
therefore difficult to deliver and maintain at sufficient bioavailability. The current formulation of many hydrophobic drugs
requires toxic solvents and surfactants such as Cremophor and Tween, which often impair drug distribution and are associated with
severe side effects. Nanomedicines, which do not require the use of toxic solvents, offer clear advantages. However, in over more than
two decades, very few nanomedicines have been successfully developed and approved for clinical use. Those already on the market
are either liposome based (such as Doxil® and Myocet®) or a protein-drug complex (such as Abraxane®). Although biodegradable
and biocompatible polymers have significant advantages over liposome and protein delivery vehicles, such as better stability and
robust molecular structure, polymeric nanoparticles have not been used beyond animal tests. Despite the great effort devoted by
many research laboratories to develop nanoformulations for drug delivery, the successful formulations after many empirical trials are
usually associated with specific compounds at a particular production scale. Reproducing the formulation at a larger scale using a
different compound was not possible. We recently developed a scalable process to generate nanoparticles encapsulating hydrophobic
compounds at high drug loading. Moreover, physicochemical properties of the particles (such as surface charge and size distribution),
which is essential for improving oral bioavailability of the compounds, can be precisely controlled by a sophisticated combination of
mixing and spray drying. Pharmacokinetics study of two hydrophobic compounds (SR13668 and curcumin) in animal models will be
demonstrated. The enhanced oral bioavailability of the compounds using polymeric nanoparticles will be presented.