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Molecules 2016, 21(1), 42;

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

Faculdade de Ciências Farmacêuticas, UNESP—University Estadual Paulista, Rodovia Araraquara Jaú Km 01, 14801-902 Araraquara, São Paulo, Brasil
Author to whom correspondence should be addressed.
Academic Editors: Thomas Rades, Holger Grohganz and Korbinian Löbmann
Received: 14 October 2015 / Revised: 10 December 2015 / Accepted: 15 December 2015 / Published: 29 December 2015
(This article belongs to the Collection Poorly Soluble Drugs)


Prodrug design is a widely known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their solubility and pharmacokinetic features and decrease their toxicity. A lack of solubility is one of the main obstacles to drug development. This review aims to describe recent advances in the improvement of solubility via the prodrug approach. The main chemical carriers and examples of successful strategies will be discussed, highlighting the advances of this field in the last ten years. View Full-Text
Keywords: prodrug; solubility; water-soluble prodrugs; solubility of prodrugs; molecular modification prodrug; solubility; water-soluble prodrugs; solubility of prodrugs; molecular modification

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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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Jornada, D.H.; dos Santos Fernandes, G.F.; Chiba, D.E.; de Melo, T.R.F.; dos Santos, J.L.; Chung, M.C. The Prodrug Approach: A Successful Tool for Improving Drug Solubility. Molecules 2016, 21, 42.

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