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Chem Sci. 2012;3(1). doi: 10.1039/C1SC00499A.

Lipid-Coated Nanoscale Coordination Polymers for Targeted Delivery of Antifolates to Cancer Cells.

Chemical science

Rachel C Huxford, Kathryn E Dekrafft, William S Boyle, Demin Liu, Wenbin Lin

Affiliations

  1. Department of Chemistry, CB#3290, University of North Carolina, Chapel Hill, NC 27599, USA ; Tel: 1-919-962-6320.

PMID: 24288587 PMCID: PMC3840543 DOI: 10.1039/C1SC00499A

Abstract

Nanoscale coordination polymers (NCPs) have been demonstrated as an interesting platform for drug delivery, as they possess many advantages over small-molecule chemotherapeutics, such as high payloads, lower systemic toxicity, tunability, and enhanced tumor uptake. Existing formulations for the delivery of methotrexate (MTX), an antifolate cancer drug, have very low drug loadings. Herein, we report the incorporation of MTX as a building block in an NCP formulation with exceptionally high drug loadings (up to 79.1 wt%) and the selective delivery of the NCP to cancer cells. Encapsulation of the NCP in a functionalized lipid bilayer allows for targeted delivery and controlled release to cancer cells. A phosphor can be doped into the NCPs for monitoring particle uptake by optical imaging. The lipid-coated and anisamide-targeted NCPs have superior

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