Abstract
Reconstituted (synthetic) high-density lipoprotein particles carrying paclitaxel (rHDL/PTX) were prepared with substantially higher PTX content than reported earlier. The rHDL/PTX complexes seemed to be primarily spherical nanoparticles when examined via electron microscopy, with a constant composition, molecular weight and exceptional stability even after ultracentrifugation and storage for up to 6 months. The rHDL/PTX nanoparticles had superior cytotoxicity against several cancer cell lines (MCF7, DU145, OV1063 and OVCAR-3), the half maximal inhibitory concentration (IC50) having been found to be 5-20 times lower than that of the free drug. Studies with mice showed that the rHDL/PTX nanoparticles were substantially better tolerated than the corresponding dosages of either Taxol or Abraxane.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents, Phytogenic / administration & dosage
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / pharmacology
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Body Weight / drug effects*
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Carbon Radioisotopes
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Cell Line, Tumor
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Cell Survival / drug effects
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Cholesterol / chemistry
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Cholesterol Esters / chemistry
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Dose-Response Relationship, Drug
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Drug Delivery Systems / methods
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Drug Evaluation, Preclinical / methods
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Female
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Humans
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Inhibitory Concentration 50
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Injections, Intraperitoneal
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Lipoproteins, HDL / chemistry*
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Mice
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Mice, Inbred C57BL
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Microscopy, Electron, Scanning
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Molecular Weight
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Nanoparticles / chemistry
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Nanoparticles / ultrastructure
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Paclitaxel / administration & dosage
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Paclitaxel / chemistry
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Paclitaxel / pharmacology*
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Particle Size
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Pharmaceutical Vehicles
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Phosphatidylcholines / chemistry
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Weight Loss / drug effects
Substances
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Antineoplastic Agents, Phytogenic
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Carbon Radioisotopes
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Cholesterol Esters
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Lipoproteins, HDL
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Pharmaceutical Vehicles
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Phosphatidylcholines
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cholesteryl oleate
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Cholesterol
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Paclitaxel