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Biodegradable Brushlike Branched Polyesters Containing a Charge-Modified Poly(vinyl alcohol) Backbone as a Platform for Drug Delivery Systems:  Synthesis and Characterization

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journal contribution
posted on 21.02.2006, 00:00 by Matthias Wittmar, Florian Unger, Thomas Kissel
Novel biodegradable, positively charged, brushlike branched polyesters, namely, poly[vinyl-3-(dialkylamino)alkylcarbamate-co-vinyl acetate-co-vinyl alcohol]-graft-poly(d,l-lactide-co-glycolide), abbreviated as (P[VACB0-70−VAc0-36−VA15-195−VPLGA75-240]), were synthesized using water-soluble amine-modified poly(vinyl alcohol) backbones in a ring opening polymerization as a platform for parenteral delivery systems of hydrophilic macromolecular drug substances such as proteins and DNA. The structure of theses graft-polyesters was studied by NMR. Modifying side chain length and charge ratio, the solubility of the polymers could be designed to range between water-soluble and lipophilic behavior. The polymers' compact, branched architecture and their molecular mass were determined by GPC-MALLS. By differential scanning calorimetry (DSC) and wide-angle X-ray scattering (WAXS) the amorphous character of the polyesters was demonstrated. The amphiphilic nature of the polyesters allowed drug entrapment by electrostatic interactions as a function of amine modification. Amine-modified graft-polyesters were shown to possess unusually short degradation times and merit further investigation as a platform for biodegradable delivery systems.