Journal of the American Chemical Society · 2005 · 276 citations · 7 references
PharmacyPharmaceuticsPharmacologyCancer PharmacologyChemotherapyDrug DeliveryCancer Drug DeliveryDrug EncapsulationLiposomal FormulationsLiposome-based DeliveryNanocarriers For TherapeuticsNanomedicineAerosol Delivery SystemsChemotherapy DeliveryDrug Delivery NanocarriersEnzymatic Drug HydrolysisEnzymatic HydrolysisLiposome Delivery SystemsLiposome Drug DeliveryLiposome-drug Conjugates
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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Cytotoxic studies of paclitaxel (Taxol®) in human tumour cell lines
J. Liebmann, J A Cook, Claudia A. Lipschultz et al. · British Journal of Cancer · 1993 · 424 citations · Full text
Medicine, Oncology, Pharmacology +14
Design, synthesis and biological activity of protaxols
K. C. Nicolaou, Claus Riemer, Michael A. Kerr et al. · Nature · 1993 · 125 citations