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A novel polyrotaxane-based intracellular delivery system for camptothecin: In vitro feasibility evaluation by Cheol Moon; Young Min Kwon; Won Kyu Lee; Yoon Jeong Park; Li-Chien Chang; Victor C. Yang is a Engineering article available to read on EtoBox.

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## Abstract Camptothecin (CPT) is a naturally occurring alkaloid that shows promise in antitumor activity __in vitro__ against various tumor cell lines. Its potential clinical uses, however, are hindered by a lack of reaction selectivity and poor water solubility. Presented herein is a novel polyrotaxane (PR)‐based delivery system that could potentially lead to a highly effective yet less toxic CPT therapy. The approach involves the synthesis of the PR–CPT conjugates via hydrolyzable linkages. To enhance the therapeutic efficacy of CPT, a cell‐penetrating peptide, LMWP, is linked to the conjugate to allow specific, intratumoral delivery of CPT. To avoid nonselective uptake of the conjugates by normal tissues following administration, the cell‐penetrating function of LMWP on the conjugates is masked by heparin binding. This system was designed such that after accumulation at the tumor via the enhanced permeability and retention (EPR) effect, protamine can be subsequently administered to unmask heparin inhibition on LMWP, permitting intracellular uptake of the LMWP–PR–CPT conjugates. Once inside the tumor, CPT molecules are detached from the PR chain by hydrolysis, yielding a sustain

Who reads A novel polyrotaxane-based intracellular delivery system for camptothecin: In vitro feasibility evaluation?

Author

Cheol Moon; Young Min Kwon; Won Kyu Lee; Yoon Jeong Park; Li-Chien Chang; Victor C. Yang

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 1549-3296)

Published

2007

Language

EN

Field

Engineering (Physical Sciences)