Patent ID: 9555011
Date: 2017-01-31
CPC Classifications: A61K,A61P,B82Y

Claim:
1. A method of making an activated targetable, loadable polymeric nanoparticle for targeted drug delivery comprising the steps of: (a) forming a first emulsion comprising a poly-lactic-co-glycolic acid biocompatible polymer in a first solvent and an active agent; (b) preparing a second solution comprising an amphiphilic polyol stabilizing agent in water, a non-solvent for the polyol, and a spacer compound selected from the group consisting of bis(sulfosuccinimidyl)suberate, ethylene glycolbis-(sulfosuccinimidylsuccinate), disuccinimidyl glutarate, N-[e-maleimidocaproyloxy] sulfosuccinimide ester, N-[b-maleimidopropyloxy] succinimide ester, and 1,8-bismaleimidodiethyleneglycol; (c) mixing the first emulsion and the second solution to form a second emulsion; (d) forming in the second emulsion an activated polymeric nanoparticle for targeted drug delivery comprising the active agent disposed within a biodegradable nanoshell comprising a poly-lactic-co-glycolic acid biocompatible polymer in contact with an amphiphilic polyol stabilizing agent and a spacer compound non-covalently sequestered in the nanoshell wall such that the electrophilic group is exposed on the exterior surface of the biodegradable nanoshell; (e) binding a targeting agent to the exposed electrophilic group, wherein the targeting agent is displayed on the exterior surface of the nanoshell; and (f) separating the activated, loaded nanoparticles.