Articles
Design Of PEG-Grafted-PLA Nanoparticles As Bioavailability Enhancer For Orally Administrated Drugs
July 23, 2009
•Poster: Design Of PEG-Grafted-PLA Nanoparticles As Bioavailability Enhancer For Orally Administrated Drugs
By Mohamed Mokhtar, Patrick Gosselin, and Patrice Hildgen
Gastrointestinal tract acts as barrier for orally administrated drugs. For drug molecules to be bioavailabile first have to across the intestinal epithelium. The tight junctions of the epithelium act as a physical barrier while the metabolic enzymes acts as biochemical barrier. In order to be absorbed, drug molecules have to be dissolved into gastrointestinal fluids, chemically stable, resistant to enzymatic degradation and not bounded to food. Moreover drug molecules need to diffuse across gastrointestinal membrane by entering epithelial cells from apical (luminal) side and exiting from basolateral or passing through the intercellular space (paracellular) to reach systemic circulation. Moreover, some drugs are affected by process known as apical efflux dependent on transporter such as P-glycoprotein (PgP). In spite of some limitations, CaCo-2 monolayer cell has been used as a tool to evaluate and test drug absorption permeability for orally administrated drugs across gastrointestinal tract. Moreover CaCo-2 monolayer cell can be used to study the major mechanism of absorption for drugs. It has been shown that CaCo-2 monolayer cell can also be used to predict the different mechanism involved in drugs to cross gastrointestinal tract into systemic circulation. PEG could be used to enhance drug bioavailability as it has been proved that it inhibits P-glycoprotein efflux. In this study Famotidine, a H2 antagonist, has been chosen as drug model because P-glycoprotein is a transporter efflux of Famotidine.
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