2008 NSTI Nanotechnology Conference and Trade Show - Nanotech 2008 - 11th Annual

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Immunomicelles for Delivery of Poorly Soluble Anticancer Drugs: Improved Solubilization and In Vitro Cytotoxicity

R.R. Sawant, V.P. Torchilin
Northeastern University, US

paclitaxel, camptothecin, immunomicelles, polyethylene glycol-phosphatidyl ethanolamine

The objective of the present work was to improve solubilization and tumor targeting of two poorly soluble anticancer drugs namely, paclitaxel and camptothecin, by mixed micelles of polyethylene glycol-phosphatidyl ethanolamine (PEG-PE) and vitamin E with coupled 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 7-25 nm and the immuno-modification of micelles did not significantly change it. Critical micelle concentration of the micelles was found to be 1.79 x 10-5 M. The solubilization of both drugs by the mixed micelles was more efficient than by micelles made of PEG-PE alone. Solubilization of camptothecin in mixed micelles prevented also the hydrolysis of active lactone form of the drug to inactive carboxylate form. The mAb 2C5 activity of immunomicelles was confirmed by ELISA using nucleosomes as antigen substrate. Drug-loaded mixed micelles and mAb 2C5-immunomicelles demonstrated significantly higher in vitro cytotoxicity than free drug against various cancer cell lines. This might be especially important for the in vivo application of immunomicelles, which combine the property of both passive tumor targeting via the EPR effect and active tumor targeting via the attached tumor-specific antibody.

Nanotech 2008 Conference Program Abstract