Nakamura Emiko, Makino Kimiko, Okano Teruo, Yamamoto Tatsuhiro, Yokoyama Masayuki
Tokyo University of Science, Department of Pharmaceutics, 2641 Yamasaki, Noda, Chiba 278-8510, Japan.
J Control Release. 2006 Sep 12;114(3):325-33. doi: 10.1016/j.jconrel.2006.05.030. Epub 2006 Jun 15.
Polymeric micelles were formed from cationic polymers (polyallylamine or protamine) and anionic block copolymers (poly(ethylene glycol)-b-poly(aspartic acid) derivative) that bound Gd ions providing high contrasts in Magnetic Resonance Imaging (MRI) by shortening the T(1) longitudinal relaxation time of protons of water. The Gd-binding block copolymer alone showed high relaxivity (T(1)-shortening ability) values from 10 to 11 mol(-1) s(-1), while the polymeric micelles exhibited low relaxivity values from 2.1 to 3.6 mol(-1) s(-1). These findings point to the feasibility of a novel MRI contrast agent that selectively provides high contrasts at solid tumor sites owing to a dissociation of the micelle structures, while selective delivery to the tumor sites is achieved in the polymeric micelle form.
聚合物胶束由阳离子聚合物(聚烯丙胺或鱼精蛋白)和阴离子嵌段共聚物(聚(乙二醇)-b-聚(天冬氨酸)衍生物)形成,这些聚合物结合钆离子,通过缩短水中质子的T(1)纵向弛豫时间在磁共振成像(MRI)中提供高对比度。单独的钆结合嵌段共聚物显示出10至11 mol(-1) s(-1)的高弛豫率(T(1)缩短能力)值,而聚合物胶束表现出2.1至3.6 mol(-1) s(-1)的低弛豫率值。这些发现表明了一种新型MRI造影剂的可行性,该造影剂由于胶束结构的解离而在实体瘤部位选择性地提供高对比度,同时以聚合物胶束形式实现对肿瘤部位的选择性递送。