Pharmacy and Pharmaceutical Sciences Commons^™

Current And Evolving Approaches For Improving The Oral Permeability Of Bcs Class Iii Or Analogous Molecules, Vivek S. Dave, Deepak Gupta, Monica Yu, Phong Nguyen, Sheeba Varghese Gupta

Pharmacy Faculty/Staff Publications

The Biopharmaceutics Classification System (BCS) classifies pharmaceutical compounds based on their aqueous solubility and intestinal permeability. The BCS Class III compounds are hydrophilic molecules (high aqueous solubility) with low permeability across the biological membranes. While these compounds are pharmacologically effective, poor absorption due to low permeability becomes the rate-limiting step in achieving adequate bioavailability. Several approaches have been explored and utilized for improving the permeability profiles of these compounds. The approaches include traditional methods such as prodrugs, permeation enhancers, ion-pairing, etc., as well as relatively modern approaches such as nanoencapsulation and nanosizing. The most recent approaches include a combination/hybridization of …