Hydrophobic oligopeptide-based star-block copolymers as unimolecular nanocarriers for poorly water-soluble drugs

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• 作者：Jinhu Li ; Jiayan Li ; Shaoqiang Xu ; D ; an Zhang ; Daojun Liu
• 关键词：Star-block copolymer ; Peptide ; Drug delivery system ; Ring-opening polymerization ; Unimolecular micelle
• 刊名：Colloids and Surfaces B: Biointerfaces
• 出版年：2013
• 出版时间：1 October, 2013
• 年：2013
• 卷：110
• 期：Complete
• 页码：183-190
• 全文大小：1349 K

文摘

Hydrophobic oligopeptide (HOP)-based star-block copolymers of the form PEI-g-(HOP-b-PEG) were synthesized, characterized and evaluated as nanocarriers for poorly water-soluble drugs. The designed PEI-g-(HOP-b-PEG) polymers were composed of a hyperbranched polyethylenimine (PEI) core, a HOP [i.e., oligo(l-tryptophan), oligo(l-phenylalanine), oligo(l-leucine), oligo(¦Ã-benzyl-l-glutamate) and oligo(?-benzyloxycarbonyl-l-lysine)] inner shell and a hydrophilic poly(ethylene glycol) (PEG) outer shell. The synthesized polymers were characterized using ¹H NMR, gel permeation chromatography (GPC) and transmission electron microscopy (TEM). Their micellization behavior was investigated by the dynamic light scattering (DLS) and fluorescence spectroscopy using pyrene as a probe; the results demonstrated that these star-block copolymers predominantly resembled unimolecular micelles, particularly when shorter HOP blocks and/or elongated PEG chains were incorporated. The encapsulation properties of these unimolecular micelles were evaluated using pyrene, oil-red O (OR) and doxorubicin (DOX) as guest hydrophobic compounds, which revealed that poorly water-soluble guests can be efficiently solubilized in PEI-g-(HOP-b-PEG) with a loading capacity of up to 10 % . The encapsulated DOX demonstrated sustained release from PEI-g-(HOP-b-PEG). The synthesized star-block copolymers, given their structural versatility, water solubility and biodegradability, could potentially be used as unimolecular nanocarriers for the delivery of poorly water-soluble drugs