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點擊次數(shù):229 發(fā)布時間:2014-12-7
文獻名:A Fullerene−Paclitaxel Chemotherapeutic: Synthesis, Characterization, and Study of Biological Activity in Tissue Culture
作者:Tatiana Y. Zakharian, Alexander Seryshev, Balaji Sitharaman, Brian E. Gilbert, Vernon Knight, and Lon J. Wilson
Department of Chemistry and the Center of Nanoscale Science and Technology, Rice University, P.O. Box 1892, Houston, Texas 77251-1892, Department of Molecular Physiology and Biophysics, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030, and Department of Molecular Virology and Microbiology, Baylor College of Medicine, One Baylor Plaza, Houston, Texas 77030
摘要: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.