Institut für Chemie und Biochemie, Freie Universität Berlin, Berlin, Germany.
Small. 2013 Mar 25;9(6):894-904. doi: 10.1002/smll.201201253. Epub 2012 Dec 6.
A new class of non-ionic dendronized multiamphiphilic polymers is prepared from a biodegradable (AB)n-type diblock polymer synthesized from 2-azido-1,3-propanediol (azido glycerol) and polyethylene glycol (PEG)-600 diethylester using Novozym-435 (Candida antarctica lipase) as a biocatalyst, following a well-established biocatalytic route. These polymers are functionalized with dendritic polyglycerols (G1 and G2) and octadecyl chains in different functionalization levels via click chemistry to generate dendronized multiamphiphilic polymers. Surface tension measurements and dynamic light scattering studies reveal that all of the multiamphiphilic polymers spontaneously self-assemble in aqueous solution. Cryogenic transmission electron microscopy further proves the formation of multiamphiphiles towards monodisperse spherical micelles of about 7-9 nm in diameter. The evidence from UV-vis and fluorescence spectroscopy suggests the effective solubilization of hydrophobic guests like pyrene and 1-anilinonaphthalene-8-sulfonic acid within the hydrophobic core of the micelles. These results demonstrate the potential of these dendronized multiamphiphilic polymers for the development of prospective drug delivery systems for the solubilization of poorly water soluble drugs.
一类新型的非离子型树枝状多两亲聚合物是由可生物降解的（AB）n 型嵌段聚合物制备的，该聚合物由 2-叠氮-1,3-丙二醇（叠氮甘油）和聚乙二醇（PEG）-600 二乙酯通过使用 Novozym-435（南极假丝酵母脂肪酶）作为生物催化剂合成，遵循一种成熟的生物催化途径。这些聚合物通过点击化学在不同的官能化水平上用树枝状聚甘油（G1 和 G2）和十八烷基链官能化，以生成树枝状多两亲聚合物。表面张力测量和动态光散射研究表明，所有的多两亲聚合物都能在水溶液中自发地自组装。低温透射电子显微镜进一步证明了形成多两亲体向单分散的约 7-9nm 直径的球形胶束的形成。紫外可见光谱和荧光光谱的证据表明，疏水性客体如芘和 1-苯胺基-8-萘磺酸能够有效地溶解在胶束的疏水性核心内。这些结果表明，这些树枝状多两亲聚合物具有用于开发有前途的药物输送系统的潜力，以溶解疏水性差的药物。
