Tuesday, 24 May 2005 - 11:00 AM

This presentation is part of: Stars, Branched, Graft and Dendritic Polymers

Conjugation of folic acid on Amphiphilic Scorpion like Macromolecules for targeting drug delivery

Jinzhong Wang, Li Tao, and Kathryn Uhrich. Rutgers, The State University of New Jersey, Piscataway, NJ

Amphiphilic Scorpion-like Macromolecules (AscMs) are amphiphilic polymeric materials designed for drug delivery applications by forming micelles in aqueous solution in our group. They are comprised of a hydrophobic part with 4 alkyl chains pendant to a central linear sugar (mucic acid) moiety and a poly (ethylene glycol) tail. The new AscM we synthesized is similar but has a primary amine group at the end of poly (ethylene glycol) tail for conjugations. For synthetic part, the four-hydroxyl groups on mucic acid are acylated by lauroyl chloride. This di-acid is selectively mono-activated by N-hydroxyl succinimide and coupled to one end of poly (ethylene glycol) bis-amine. The AScMs aggregate to form micelles at very low concentrations below 1 ÁM. the micelle size is about 15nm, small enough to avoid rapid clearance by reticuloendothelial system (RES). Drug loading of the control AScMs with an anti-cancer drug ellipticine is as high as 30% weight percent and efficiency can reach up to 94 percent. Folic acid activated by N-hydroxyl succinimide is conjugated with the amine group on the poly (ethylene glycol) tail. The conjugation process is followed by HPLC and GPC spectroscopy. The in vitro study using A 2780 cancer cell line with ellipticin is under way.

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