Next Article in Journal
Diversity-Oriented Synthesis as a Tool for Chemical Genetics
Next Article in Special Issue
Anti-Obesity Effects of Hispidin and Alpinia zerumbet Bioactives in 3T3-L1 Adipocytes
Previous Article in Journal
Design of Composite Photocatalyst of TiO2 and Y-Zeolite for Degradation of 2-Propanol in the Gas Phase under UV and Visible Light Irradiation
Previous Article in Special Issue
Exploration of Piperidinols as Potential Antitubercular Agents
Article Menu
Issue 10 (October) cover image

Export Article

Open AccessConcept Paper
Molecules 2014, 19(10), 16489-16505;

Modern Prodrug Design for Targeted Oral Drug Delivery

Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva 84105, Israel
Department of Medicine, Division of Gastroenterology, University of Florida, Gainesville, FL 32608, USA
Author to whom correspondence should be addressed.
Received: 12 September 2014 / Revised: 7 October 2014 / Accepted: 8 October 2014 / Published: 14 October 2014
(This article belongs to the Special Issue Prodrugs)
Full-Text   |   PDF [1207 KB, uploaded 14 October 2014]   |  


The molecular information that became available over the past two decades significantly influenced the field of drug design and delivery at large, and the prodrug approach in particular. While the traditional prodrug approach was aimed at altering various physiochemical parameters, e.g., lipophilicity and charge state, the modern approach to prodrug design considers molecular/cellular factors, e.g., membrane influx/efflux transporters and cellular protein expression and distribution. This novel targeted-prodrug approach is aimed to exploit carrier-mediated transport for enhanced intestinal permeability, as well as specific enzymes to promote activation of the prodrug and liberation of the free parent drug. The purpose of this article is to provide a concise overview of this modern prodrug approach, with useful successful examples for its utilization. In the past the prodrug approach used to be viewed as a last option strategy, after all other possible solutions were exhausted; nowadays this is no longer the case, and in fact, the prodrug approach should be considered already in the very earliest development stages. Indeed, the prodrug approach becomes more and more popular and successful. A mechanistic prodrug design that aims to allow intestinal permeability by specific transporters, as well as activation by specific enzymes, may greatly improve the prodrug efficiency, and allow for novel oral treatment options. View Full-Text
Keywords: molecular biopharmaceutics; membrane transporters; passive/active intestinal permeability; prodrug activation; targeted prodrug approach molecular biopharmaceutics; membrane transporters; passive/active intestinal permeability; prodrug activation; targeted prodrug approach

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Dahan, A.; Zimmermann, E.M.; Ben-Shabat, S. Modern Prodrug Design for Targeted Oral Drug Delivery. Molecules 2014, 19, 16489-16505.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top