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. 2005 Sep 14;127(36):12508-9.
doi: 10.1021/ja0546525.

A fullerene-paclitaxel chemotherapeutic: synthesis, characterization, and study of biological activity in tissue culture

Tatiana Y Zakharian  1 , Alexander Seryshev, Balaji Sitharaman, Brian E Gilbert, Vernon Knight, Lon J Wilson
Affiliations

A fullerene-paclitaxel chemotherapeutic: synthesis, characterization, and study of biological activity in tissue culture

Tatiana Y Zakharian et al. J Am Chem Soc. .

Abstract

A fullerene-paclitaxel conjugate has been synthesized as a slow-release drug for aerosol liposome delivery of paclitaxel for lung cancer therapy. The conjugate was designed to release paclitaxel via enzymatic hydrolysis and subsequently has shown a half-life of release of 80 min in bovine plasma. A liposome formulation of the conjugate has been prepared using dilauroylphosphatidylcholine (DLPC), and its IC50 is virtually identical to the IC50 for a paclitaxel-DLPC formulation in human epithelial lung carcinoma A549 cells. With both clinically relevant kinetics of hydrolysis and significant cytotoxicity in tissue culture, the conjugate holds promise for enhanced therapeutic efficacy of paclitaxel in vivo.

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