@article { ISI:000269988600011,
	title = {Fullerenol-cytotoxic conjugates for cancer chemotherapy},
	journal = {ACS Nano},
	volume = {3},
	number = {9},
	year = {2009},
	month = {SEP},
	pages = {2505-2514},
	publisher = {AMER CHEMICAL SOC},
	address = {1155 16TH ST, NW, WASHINGTON, DC 20036 USA},
	abstract = {<p>In the present study, we report the novel application of polyhydroxylated fullerenes (fullerenols) in cancer drug delivery. The facile synthetic procedure for generating multiple hydroxyl groups on the fullerene cage offers scope for high drug loading in addition to conferring hydrophilicity. Doxorubicin, a first line cancer chemotherapeutic, was conjugated to fullerenols through a carbamate linker, achieving ultrahigh loading efficiency. The drug-fullerenol conjugate was found to be relatively stable in phosphate buffer saline but temporally released the active drug when incubated with tumor cell lysate. The fullerenol-doxorubicin conjugate suppressed the proliferation of cancer cell-lines in vitro through a G2-M cell cycle block, resulting in apoptosis. Furthermore, in an in vivo murine tumor model, fullerenol-doxorubicin exhibited Comparable antitumor efficacy as free drug without the systemic toxicity of free doxorubicin. Additionally, we demonstrate that the fullerenol platform can be extended to other chemotherapeutic agents, such as the slightly water-soluble cisplatin, and can emerge as a new paradigm in the management of cancer.</p>},
	keywords = {chemotherapy, doxorubicin, drug delivery, fullerenol, nanoparticle},
	issn = {1936-0851},
	doi = {10.1021/nn900318y},
	author = {Chaudhuri, Padmaparna and Paraskar, Abhimanyu and Soni, Shivani and Mashelkar, Raghunath Anant and Sengupta, Shiladitya}
}
@article { ISI:000279843200010,
	title = {Harnessing structure-activity relationship to engineer a cisplatin nanoparticle for enhanced antitumor efficacy},
	journal = {Proceedings of the National Academy of Sciences of the United States of America},
	volume = {107},
	number = {28},
	year = {2010},
	month = {JUL},
	pages = {12435-12440},
	publisher = {NATL ACAD SCIENCES},
	address = {2101 CONSTITUTION AVE NW, WASHINGTON, DC 20418 USA},
	abstract = {<p>Cisplatin is a first line chemotherapy for most types of cancer. However, its use is dose-limited due to severe nephrotoxicity. Here we report the rational engineering of a novel nanoplatinate inspired by the mechanisms underlying cisplatin bioactivation. We engineered a novel polymer, glucosamine-functionalized polyisobutylene-maleic acid, where platinum (Pt) can be complexed to the monomeric units using a monocarboxylato and an O {\textendash}\&gt; Pt coordinate bond. We show that at a unique platinum to polymer ratio, this complex self-assembles into a nanoparticle, which releases cisplatin in a pH-dependent manner. The nanoparticles are rapidly internalized into the endolysosomal compartment of cancer cells, and exhibit an IC50 (4.25 + 0.16 mu M) comparable to that of free cisplatin (3.87 +/- 0.37 mu M), and superior to carboplatin (14.75 +/- 0.38 mu M). The nanoparticles exhibited significantly improved antitumor efficacy in terms of tumor growth delay in breast and lung cancers and tumor regression in a K-ras(LSL/+)/Pten(fl/fl) ovarian cancer model. Furthermore, the nanoparticle treatment resulted in reduced systemic and nephrotoxicity, validated by decreased biodistribution of platinum to the kidney as quantified using inductively coupled plasma spectroscopy. Given the universal need for a better platinate, we anticipate this coupling of nanotechnology and structure-activity relationship to rationally reengineer cisplatin could have a major impact globally in the clinical treatment of cancer.</p>},
	keywords = {cancer, chemotherapy, nanomedicine},
	issn = {0027-8424},
	doi = {10.1073/pnas.1007026107},
	author = {Paraskar, Abhimanyu S. and Soni, Shivani and Chin, Kenneth T. and Chaudhuri, Padmaparna and Muto, Katherine W. and Berkowitz, Julia and Handlogten, Michael W. and Alves, Nathan J. and Bilgicer, Basar and Dinulescu, Daniela M. and Mashelkar, Raghunath Anant and Sengupta, Shiladitya}
}
