Exploiting EPR in Polymer Drug Conjugate Delivery for Tumor Targeting

Authors: Modi, Sweta; Prakash Jain, Jay; Domb, A. J.; Kumar, Neeraj

Source: Current Pharmaceutical Design, Volume 12, Number 36, December 2006 , pp. 4785-4796(12)

Publisher: Bentham Science Publishers

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Abstract:

Treatment of tumor tissue without affecting normal cells has always been formidable task for drug delivery scientists and this task is effectively executed by polymer drug conjugate (PDC) delivery. The novelty of this concept lies in the utilization of a physical mechanism called enhanced permeability and retention (EPR) for targeting tumors. EPR is a physiological phenomenon that is customary for fast growing tumor and solves the problem of targeting the miscreant tissue. PDCs offer added advantages of reduced deleterious effects of anticancer drugs and augmentation of its formulation capability (e.g. Solubility). There are now at least eleven PDCs that have entered phase I/II/III clinical trial as anticancer drugs. PDCs once entered into the tumor tissue, taking advantage of EPR, are endocytosed into the cell either by simple or receptor mediated endocytosis. Various polymeric carriers have been used with hydrolyzable linker arm for conjugation with bioactive moiety. The hydrolyzable linkages of PDC are broken down by acid hydrolyses of lysosomes and releases the drug. High concentrations of the chemotherapeutic agent are maintained near the nucleus, the target site. Passive targeting by PDCs is due to the physiological event of EPR, which is becoming one of the major thrust areas for targeting solid tumors.

Keywords: EPR; polymer-drug conjugates; cancer; targeting; linkers; endocytosis; PEGylation; HPMA

Document Type: Research article

DOI: http://dx.doi.org/10.2174/138161206779026272

Affiliations: 1: Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Sec. 67, S.A.S. Nagar (Mohali) - 160062, India.

Publication date: 2006-12-01

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Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

Exploiting EPR in Polymer Drug Conjugate Delivery for Tumor Targeting

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