Synthesis and self-assembly of RGD-functionalized PEO-PB amphiphiles.
Synthesis and self-assembly of RGD-functionalized PEO-PB amphiphiles.
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DOI：
10.1021/bm900149b
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发表时间：
2009-06-08
影响因子：
6.2
通讯作者：
Hillmyer, Marc A.
中科院分区：
文献类型：
--
作者：
Zupancich, John A.;Bates, Frank S.;Hillmyer, Marc A.
两亲嵌段共聚物自组装提供了一种在溶液中制备纳米级胶束的通用方法。利用这些结构作为靶向药物递送载体激发了制备生物活性配体功能化聚合物胶束的努力。配体共轭对胶束形态的影响通过使用表征良好的聚环氧乙烷-b-聚丁二烯（OB）嵌段共聚物进行了研究，这些共聚物在不同程度上功能化了与生物相关的含rgd肽序列。采用低温透射电镜（cryo-TEM）和动态力学分析研究了RGD-OB共聚物的胶束形态和稀溶液行为。RGD-OB共聚物在去离子水中的直接分散产生了多种结构；观察到的形态偏离了由肽偶联引起的两亲化合物组成的总体变化所预测的规范序列。制备了RGD功能化的球形胶束、圆柱形胶束网络和环形多层囊泡。这种形态行为归因于结合到冠状链末端的肽段之间的相互作用，并对药物递送应用的靶向胶束设计具有指导意义。
Amphiphilic block copolymer self-assembly provides a versatile means to prepare nanoscale micelles in solution. The utilization of these structures as targeted drug delivery vehicles has motivated efforts to prepare bioactive ligand-functionalized polymer micelles. The impact of ligand conjugation on micelle morphology was examined through use of well-characterized poly(ethylene oxide)-b-poly(butadiene) (OB) block copolymers functionalized to varying extents with a biologically relevant RGD-containing peptide sequence. Micelle morphology and dilute solution behavior of RGD-functionalized OB (RGD-OB) copolymers were examined using cryogenic transmission electron microscopy (cryo-TEM) and dynamic mechanical analysis. The direct dispersion of RGD-OB copolymers into deionized water yielded a variety of structures; the observed morphologies deviated from the canonical series predicted by the overall change in amphiphile composition due to peptide conjugation. RGD functionalized spherical micelles, cylindrical micelle networks and annular multilayer vesicles were prepared. The morphological behavior was attributed to interactions between peptide moieties conjugated to the termini of coronal chains and has implications in the design of targeting micelles for drug delivery applications.
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