Zupancich John A, Bates Frank S, Hillmyer Marc A
Department of Chemical Engineering, University of Minnesota, Minneapolis, Minnesota 55455-0431, USA.
Biomacromolecules. 2009 Jun 8;10(6):1554-63. doi: 10.1021/bm900149b.
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.
两亲性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。将这些结构用作靶向药物递送载体促使人们努力制备生物活性配体功能化的聚合物胶束。通过使用具有良好表征的聚环氧乙烷-b-聚丁二烯（OB）嵌段共聚物，该共聚物用含有生物相关RGD的肽序列进行不同程度的功能化，研究了配体共轭对胶束形态的影响。使用低温透射电子显微镜（cryo-TEM）和动态力学分析研究了RGD功能化的OB（RGD-OB）共聚物的胶束形态和稀溶液行为。将RGD-OB共聚物直接分散到去离子水中产生了多种结构；观察到的形态偏离了由于肽共轭导致两亲物组成的总体变化所预测的典型系列。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。形态行为归因于与冠状链末端共轭的肽部分之间的相互作用，并且对用于药物递送应用的靶向胶束的设计具有影响。
