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Molecules 2014, 19(12), 20780-20807; doi:10.3390/molecules191220780

Prodrug Strategies for Enhancing the Percutaneous Absorption of Drugs

Centre of Excellence for Pharmaceutical Sciences (PHARMACEN), North-West University, Potchefstroom 2520, South Africa
Received: 20 October 2014 / Revised: 3 December 2014 / Accepted: 4 December 2014 / Published: 12 December 2014
(This article belongs to the Special Issue Prodrugs)
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Abstract

The transdermal application of drugs has attracted increasing interest over the last decade or so, due to the advantages it offers, compared to other delivery methods. The development of an efficient means of transdermal delivery can increase drug concentrations, while reducing their systemic distribution, thereby avoiding certain limitations of oral administration. The efficient barrier function of the skin, however, limits the use of most drugs as transdermal agents. This limitation has led to the development of various strategies to enhance drug-skin permeation, including the use of penetration enhancers. This method unfortunately has certain proven disadvantages, such as the increased absorption of unwanted components, besides the drug, which may induce skin damage and irritancy. The prodrug approach to increase the skin’s permeability to drugs represents a very promising alternative to penetration enhancers. The concept involves the chemical modification of a drug into a bioreversible entity that changes both its pharmaceutical and pharmacokinetic characteristics to enhance its delivery through the skin. In this review; we report on the in vitro attempts and successes over the last decade by using the prodrug strategy for the percutaneous delivery of pharmacological molecules. View Full-Text
Keywords: prodrug; percutaneous absorption; enhancer; transdermal penetration prodrug; percutaneous absorption; enhancer; transdermal penetration
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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).

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N'Da, D.D. Prodrug Strategies for Enhancing the Percutaneous Absorption of Drugs. Molecules 2014, 19, 20780-20807.

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