Surface-modified nanoparticles for intracellular delivery of therapeutic agents and composition for making same

摘要

Surface-modified polymeric nanoparticles (NPs), compositions for making them, and their use in drug delivery are disclosed.

主权项

1. A surface modified nanoparticle for delivery of therapeutic agents, said surface modified nanoparticle comprising (i) a biocompatible polymer (ii) an amphiphilic emulsifier and (iii) a charge modulator, wherein said biocompatible polymer is poly(lactide-co-glycolide), said amphiphilic emulsifier is polyvinyl alcohol and said charge modulator is poly-L-lysine, (i), (ii) and (iii) forming a nanoparticle matrix, the weight ratio of said amphiphilic emulsifier to said charge modulator from which said nanoparticle is prepared is in the range of 4:1 to 1.5:1, said nanoparticle having a negative surface charge at neutral pH, said charge modulator being embedded in said nanoparticle matrix and extending from the nanoparticle surface, and said charge modulator being effective to reverse said surface charge from negative to positive in an acidic environment, thereby improving the efficiency of intracellular delivery of therapeutic agents carried by said nanoparticle, said surface modified nanoparticle having a greater force of adhesion to a cell membrane for enhancing cellular uptake of said nanoparticle as compared to an unmodified nanoparticle comprising said biocompatible polymer and said amphiphilic emulsifier without said charge modulator.