Lysine-block-tyrosine block copolypeptides: Self-assembly, cross-linking, and conjugation of targeted ligand for drug encapsulation

Lysine-block-tyrosine block copolypeptides: Self-assembly, cross-linking, and conjugation of targeted ligand for drug encapsulation
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DOI:
10.1016/j.polymer.2012.01.010
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发表时间:
2012-02-17
期刊:
影响因子:
4.6
通讯作者:
Jan, Jeng-Shiung
Jan, Jeng-Shiung
中科院分区:
化学2区
文献类型:
--
作者:
Huang, Yun-Chiao;Yang, Yao-Sheng;Jan, Jeng-Shiung

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本文报道了聚L-赖氨酸-聚L-酪氨酸(PLL-b-PLT)嵌段多肽的合成及自组装。这些嵌段共聚肽自组装形成囊泡或胶束的大小在100和350 nm之间的光散射和电子显微镜证实。通过紫外维斯、荧光光谱和圆二色谱研究了嵌段多肽的光谱性质和链构象。UV交联的胶束和囊泡可以通过酪氨酸残基的二聚化来制备,通过在410-430 nm处的荧光发射的存在来证明。嵌段共聚肽可以通过多种细胞靶向配体官能化,如通过糖基、乳糖内酯缀合到共聚物上所证明的。初步评价了糖肽的体外释药性能。由于PLL和PLT片段表现出的独特功能,可以预期这些两亲性嵌段共聚肽可用作生物医学领域的靶向药物载体、功能性纳米生物反应器和仿生澄清剂。(C)2012爱思唯尔有限公司保留所有权利。
This report describes the synthesis and self-assembly of poly(L-lysine)-block-poly(L-tyrosine) (PLL-b-PLT) block copolypeptides. These block copolypeptides self-assembled to form vesicles or micelles with sizes between 100 and 350 nm as confirmed by light scattering and electron microscopy. The spectral properties and chain conformation of these block copolypeptides were studied by UV/vis, fluorescence, and circular dichroism. UV cross-linked micelles and vesicles can be prepared by dimerization of tyrosine residues, evidenced by the presence of fluorescence emission at 410-430 nm. The block copolypeptides can be functionalized by a variety of cell-targeted ligands as demonstrated by conjugation of a saccharide group, lactobionolactone, onto the copolymers. A preliminary evaluation of the glycopeptides for in vitro drug release was studied. Due to the unique features exhibited by both PLL and PLT segments, it can be expected that these amphiphilic block copolypeptides to be useful as targeted drug carriers, functional nanobioreactors, and biomimetic encapsulants in the biomedical fields. (C) 2012 Elsevier Ltd. All rights reserved.