Self-assembled polypeptide-block-poly(vinylpyrrolidone) as prospective drug-delivery systems

Lei Wang, Rong Zeng, Chao Li, Renzhong Qiao, Lei Wang, Rong Zeng, Chao Li, Renzhong Qiao

Index: Colloids Surf. B Biointerfaces 74 , 284-292, (2009)

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Abstract

Poly(β-benzyl- l-aspartate)- block-poly(vinylpyrrolidone) diblock copolymers (PAsp(OBzl)- b-PVP) having both hydrophobic and hydrophilic segments of various lengths were synthesized by a combination of ATRP and ROP. These amphiphilic diblock copolymers formed polymeric micelles consisting of a hydrophobic PAsp(OBzl) core and a hydrophilic PVP shell in aqueous solution. The block copolymer was characterized using 1H NMR and gel permeation chromatography (GPC) analysis. Due to its core–shell structure, this block polymer forms unimolecular micelles in aqueous solutions. The micelle properties of PAsp(OBzl)- b-PVP diblock copolymer were extensively studied by dynamic light scattering (DLS), fluorescence spectroscopy, and transmission electron microscopy (TEM). PAsp(OBzl)- b-PVP copolymers displayed the lowest CMC and demonstrated little cytotoxicity when exposed to SW-1990 pancreatic cancer cells. In order to assess its application in biomedical area, the anti-inflammation drug prednisone acetate was loaded as the model drug in the polymeric nanoparticles. In vitro release behavior of prednisone acetate was investigated, which showed a dramatic responsive fast/slow switching behavior according to the pH-responsive structural changes of a micelle core structure. All of theses features are quite feasible for utilizing it as a novel intelligent drug-delivery system.