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Polymer-Based Prodrugs: Improving Tumor Targeting and the Solubility of Small Molecule Drugs in Cancer Therapy

Department of Biochemistry, University of Mississippi Medical Center, 2500 North State Street Jackson, MS 39216, USA
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Academic Editors: Thomas Rades, Holger Grohganz and Korbinian Löbmann
Molecules 2015, 20(12), 21750-21769; https://doi.org/10.3390/molecules201219804
Received: 25 September 2015 / Revised: 5 November 2015 / Accepted: 17 November 2015 / Published: 4 December 2015
(This article belongs to the Collection Poorly Soluble Drugs)
The majority of anticancer drugs have poor aqueous solubility, produce adverse effects in healthy tissue, and thus impose major limitations on both clinical efficacy and therapeutic safety of cancer chemotherapy. To help circumvent problems associated with solubility, most cancer drugs are now formulated with co-solubilizers. However, these agents often also introduce severe side effects, thereby restricting effective treatment and patient quality of life. A promising approach to addressing problems in anticancer drug solubility and selectivity is their conjugation with polymeric carriers to form polymer-based prodrugs. These polymer-based prodrugs are macromolecular carriers, designed to increase the aqueous solubility of antitumor drugs, can enhance bioavailability. Additionally, polymer-based prodrugs approach exploits unique features of tumor physiology to passively facilitate intratumoral accumulation, and so improve chemodrug pharmacokinetics and pharmacological properties. This review introduces basic concepts of polymer-based prodrugs, provides an overview of currently emerging synthetic, natural, and genetically engineered polymers that now deliver anticancer drugs in preclinical or clinical trials, and highlights their major anticipated applications in anticancer therapies. View Full-Text
Keywords: polymer based prodrugs; anticancer drugs; macromolecules; drug delivery; cancer therapy; genetically engineered biopolymers; synthetic and natural polymers polymer based prodrugs; anticancer drugs; macromolecules; drug delivery; cancer therapy; genetically engineered biopolymers; synthetic and natural polymers
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Dragojevic, S.; Ryu, J.S.; Raucher, D. Polymer-Based Prodrugs: Improving Tumor Targeting and the Solubility of Small Molecule Drugs in Cancer Therapy. Molecules 2015, 20, 21750-21769.

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