Mixed PEG-PE/vitamin E tumor-targeted immunomicelles as carriers for poorly soluble anti-cancer drugs: improved drug solubilization and enhanced in vitro cytotoxicity.

Abstract	Two poorly soluble, potent anti-cancer drugs, paclitaxel and camptothecin, were successfully solubilized by mixed micelles of polyethylene glycol-phosphatidyl ethanolamine (PEG-PE) and vitamin E. Drug-containing micelles were additionally modified with anti-nucleosome monoclonal antibody 2C5 (mAb 2C5), which can specifically bring micelles to tumor cells in vitro. The optimized micelles had an average size of about 13-22 nm and the immuno-modification of micelles did not significantly change it. The solubilization of both drugs by the mixed micelles was more efficient than by micelles made of PEG-PE alone. Solubilization of camptothecin in micelles prevented also the hydrolysis of active lactone form of the drug to inactive carboxylate form. Drug-loaded mixed micelles and mAb 2C5-immunomicelles demonstrated significantly higher in vitro cytotoxicity than free drug against various cancer cell lines.
Authors	Rupa R Sawant, Rishikesh M Sawant, Vladimir P Torchilin
Journal	European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V (Eur J Pharm Biopharm) Vol. 70 Issue 1 Pg. 51-7 (Sep 2008) ISSN: 0939-6411 [Print] Netherlands
PMID	18583114 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
Chemical References	Antibodies, Monoclonal Antineoplastic Agents, Phytogenic Drug Carriers Micelles Nucleosomes Phosphatidylethanolamines polyethylene glycol-distearoylphosphatidylethanolamine Vitamin E Polyethylene Glycols Paclitaxel Camptothecin
Topics	Animals Antibodies, Monoclonal (chemistry, metabolism) Antineoplastic Agents, Phytogenic (chemistry, metabolism, pharmacology) Camptothecin (chemistry, metabolism, pharmacology) Cell Line, Tumor Cell Survival (drug effects) Chemistry, Pharmaceutical Dose-Response Relationship, Drug Drug Carriers Drug Stability Hydrolysis Mice Micelles Nucleosomes (immunology) Paclitaxel (chemistry, metabolism, pharmacology) Particle Size Phosphatidylethanolamines (chemistry) Polyethylene Glycols (chemistry) Solubility Technology, Pharmaceutical (methods) Time Factors Vitamin E (chemistry)

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