Optimizing polymer compositions leads to optimum drug delivery with biodegradable self-assembling block copolymer nanospheres

COLL 109

Larisa Sheihet, Robert A. Dubin, Karolina Piotrowska, piotrowska@biology.rutgers.edu, Joachim Kohn, kohn@biology.rutgers.edu, and David I. Devore. New Jersey Center for Biomaterials, Rutgers, State University of New Jersey, 145 Bevier Road, Piscataway, NJ 08854
To overcome the obstacles of poor bioavailability, circulation time and cell permeability that limit the delivery and efficacy of many hydrophobic therapeutic compounds, we have designed and synthesized amphiphilic ABA-type triblock copolymers that self-assemble into nanopheres with desaminotyrosyl-tyrosine ester cores and poly(ethylene oxide) shells. These biocompatible copolymers provide a unique tunability that we exploit to obtain structure-activity relationships for a subset of nanosphere architectures and apply these to optimize their drug loading capabilities. We calculate thermodynamic solubility parameters for drugs with a range of hydrophobicities to provide an understanding of their binding and release from the nanospheres under dialysis conditions. Finally, we demonstrate that the optimized nanospheres deliver the hydrophobic anti-tumor drugs, paclitaxel and camptothecin, to human tumor cells in vitro with no loss of drug activity.
 

Advances in Nanomedicine
2:00 PM-5:30 PM, Sunday, 10 September 2006 Sir Francis Drake -- Monterey/Cypress Rooms, Oral

Division of Colloid & Surface Chemistry

The 232nd ACS National Meeting, San Francisco, CA, September 10-14, 2006