Rationally engineered polymeric cisplatin nanoparticles for improved antitumor efficacy

Abhimanyu Paraskar, Shivani Soni, Sudipta Basu, Chitra J. Amarasiriwardena, Nicola Lupoli, Shyam Srivats, Rituparna Sinha Roy, Shiladitya Sengupta

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29 Scopus citations


The use of cisplatin, a first line chemotherapy for most cancers, is dose-limited due to nephrotoxicity. While this toxicity can be addressed through nanotechnology, previous attempts at engineering cisplatin nanoparticles have been limited by the impact on the potency of cisplatin. Here we report the rational engineering of a novel cisplatin nanoparticle by harnessing a novel polyethylene glycol-functionalized poly-isobutylene-maleic acid (PEG-PIMA) copolymer, which can complex with cis-platinum (II) through a monocarboxylato and a coordinate bond. We show that this complex self-assembles into a nanoparticle, and exhibits an IC50 = 0.77 0.11νM comparable to that of free cisplatin (IC50 = 0.44 0.09νM). The nanoparticles are internalized into the endolysosomal compartment of cancer cells, and release cisplatin in a pH-dependent manner. Furthermore, the nanoparticles exhibit significantly improved antitumor efficacy in a 4T1 breast cancer model invivo, with limited nephrotoxicity, which can be explained by preferential biodistribution in the tumor with reduced kidney concentrations. Our results suggest that the PEG-PIMA-cisplatin nanoparticle can emerge as an attractive solution to the challenges in cisplatin chemotherapy.

Original languageEnglish
Article number265101
Issue number26
StatePublished - 1 Jul 2011
Externally publishedYes


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