Department of Chemistry, University of Athens, Greece.
Biomacromolecules. 2010 Feb 8;11(2):430-8. doi: 10.1021/bm901151g.
We synthesized a series of well-defined poly(dl-lactide)-b-poly(N,N-dimethylamino-2-ethyl methacrylate) (PDLLA-b-PDMAEMA) amphiphilic diblock copolymers by employing a three-step procedure: (a) ring-opening polymerization (ROP) of dl-lactide using n-decanol and stannous octoate, Sn(Oct)(2), as the initiating system, (b) reaction of the PDLLA hydroxyl end groups with bromoisobutyryl bromide, and (c) atom transfer radical polymerization, ATRP, of DMAEMA with the newly created bromoisobutyryl initiating site. The aggregation behavior of the prepared block copolymers was investigated by dynamic light scattering and zeta potential measurements at 25 degrees C in aqueous solutions of different pH values. The hydrophobic drug dipyridamole was efficiently incorporated into the copolymer aggregates in aqueous solutions of pH 7.40. High partition coefficient values were determined by fluorescence spectroscopy.
我们通过三步法合成了一系列结构明确的聚(DL-丙交酯)-b-聚(N,N-二甲基氨基-2-乙基甲基丙烯酸酯)(PDLLA-b-PDMAEMA)两亲性嵌段共聚物:(a)使用正癸醇和辛酸亚锡(Sn(Oct)(2))作为引发体系,通过开环聚合(ROP)聚合 DL-丙交酯,(b)PDLLA 羟基端基与溴代异丁酰溴反应,以及(c)在新生成的溴代异丁酰引发位点上进行 DMAEMA 的原子转移自由基聚合(ATRP)。在不同 pH 值的水溶液中,通过动态光散射和 zeta 电位测量研究了所制备的嵌段共聚物的聚集行为。疏水性药物双嘧达莫在 pH 值为 7.40 的共聚物水溶液中被有效包裹。通过荧光光谱法测定了高分配系数值。