title: Current and evolving approaches for improving the oral permeability of BCS Class III or analogous molecules.
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.
authors.affiliation: a Wegmans School of Pharmacy , St. John Fisher College , Rochester , NY , USA.
authors.forename: Vivek S
authors.initials: VS
authors.lastname: Dave
authors.affiliation: b Lake Eerie College of Osteopathic Medicine , School of Pharmacy, Pharmaceutical Sciences , Bradenton , FL , USA.
authors.forename: Deepak
authors.initials: D
authors.lastname: Gupta
authors.affiliation: b Lake Eerie College of Osteopathic Medicine , School of Pharmacy, Pharmaceutical Sciences , Bradenton , FL , USA.
authors.forename: Monica
authors.initials: M
authors.lastname: Yu
authors.affiliation: b Lake Eerie College of Osteopathic Medicine , School of Pharmacy, Pharmaceutical Sciences , Bradenton , FL , USA.
authors.forename: Phuong
authors.initials: P
authors.lastname: Nguyen
authors.affiliation: c Department of Pharmaceutical Sciences , USF College of Pharmacy , Tampa , FL , USA.
authors.forename: Sheeba
authors.initials: S
authors.lastname: Varghese Gupta
mesh_terms: D001682:Biological Availability; D001702:Biopharmaceutics / Q000145:classification / Q000592:standards*; D055808:Drug Discovery; D057927:Hydrophobic and Hydrophilic Interactions; D010539:Permeability; D012995:Solubility; D014481:United States; D014486:United States Food and Drug Administration
keywords: BCS Class III; Permeability; counterion; ion-pairing; liposome; nanotechnology; permeation enhancer; prodrugs