Document Type
Article
Publication Date
12-20-2016
Keywords
Permeability, BCS Class III, Prodrugs, Ion-pairing, Counterion, Nanotechnology, Liposome, Permeation enhancer
Abstract
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 one or more traditional approaches to improve drug permeability. While some of these approaches have been extremely successful, i.e. drug products utilizing the approach have progressed through the USFDA approval for marketing; others require further investigation to be applicable. This article discusses the commonly studied approaches for improving the permeability of BCS Class III compounds.
DOI
10.1080/03639045.2016.1269122
Publication Information
Dave, Vivek S.; Gupta, Deepak; Yu, Monica; Nguyen, Phong; and Gupta, Sheeba Varghese (2016). "Current and evolving approaches for improving the oral permeability of BCS Class III or analogous molecules." Drug Development and Industrial Pharmacy 43.2, 177-189.
Please note that the Publication Information provides general citation information and may not be appropriate for your discipline. To receive help in creating a citation based on your discipline, please visit http://libguides.sjfc.edu/citations.
Comments
This is an Accepted Manuscript of an article published by Taylor & Francis in Drug Development and Industrial Pharmacy on December 20, 2016, available online: http://www.tandfonline.com/10.1080/03639045.2016.1269122.