Research in formulation of poorly watersoluble active compounds in PLGA Nanoparticles using spray-drying technology.

The poor water-solubility of new active pharmaceutical ingredients (API) is a true challenge for formulation experts. Before an API can reach the systemic circulation and reach the target site of action, orally-taken drugs need to dissolve first in the gastrointestinal fluids. The use of organic solvents in high-throughput screening of new API's, as well as the structure-activity related research, often results in candidate-molecules with an extreme lipophilicity and high molecular weight and consequently a poor water-solubility. In this project, different formulation technologies will be screened to increase the bio-availability of these API's. This project focusses on an innovative technology, the spray-drying of nanoparticles (NP's), in comparison with 3 more conventional formulation approaches (cyclodextrine-complexes, amorphous systems and PolyLactic-co-Glycolic Acid (PLGA)-nanoparticles).Embeded in the Antwerp Drug Discovery Network of the UA, the Laboratory of Pharmaceutical Technology (LPTB) is well situated to bridge the Medicinal Chemistry research activities with the LMPH in vivo-modeling expertise. This allows the evaluation of the full potential of new medicinal compounds in an in vitro and in vivo setting. Last year, the applicants' laboratory supported several other UA labs requesting formulation assistance with their poorly water-soluble compounds.

Keywords:NANOPARTICLES, SPRAY DRYING, SOLUBILITY, FORMULATION

Disciplines:Biomarker discovery and evaluation, Drug discovery and development, Medicinal products, Pharmaceutics, Pharmacognosy and phytochemistry, Pharmacology, Pharmacotherapy, Toxicology and toxinology, Other pharmaceutical sciences