National Synchrotron Radiation Lab and College of Nuclear Science and Technology, University of Science and Technology of China, Hefei, 230026, People's Republic of China.
J Mater Sci Mater Med. 2010 Feb;21(2):557-65. doi: 10.1007/s10856-009-3880-4. Epub 2009 Sep 26.
A series of amphiphilic N-phthaloylchitosan-g-polycaprolactone molecular bottle brushes were prepared by "graft onto" method. The narrow distribution of polycaprolactone macromonomers ensures that the molecular bottle brushes can self-assemble into highly monodisperse particles, which have the ability to get a high loading efficiency of the hydrophobic drug, indometacin (INN). Searching for the effective drug loading ratio, three parameters such as polycaprolactone chain length, the grafting content and concentration of the molecular bottle brushes were tested to entrap INN. These encapsulated drug particles show sustained release of the encapsulated INN, of which 91.7% was released in 22 h at 37 degrees C in phosphate buffered saline. The self-assembled particles of the molecular bottle brushes as carriers for INN can effectively prevent the drug from releasing quickly and prolong the release time, which is a promising candidate for potential clinical applications.
一系列的两亲性 N-邻苯二甲酰壳聚糖-g-聚己内酯分子瓶刷是通过“接枝到”的方法制备的。聚己内酯大分子单体的窄分布确保了分子瓶刷可以自组装成高度单分散的颗粒，具有获得疏水性药物吲哚美辛（INN）的高载药效率的能力。为了寻找有效的药物载药率，测试了聚己内酯链长、接枝含量和分子瓶刷浓度这三个参数来包载 INN。这些包封药物颗粒显示出包封 INN 的持续释放，在 37°C 磷酸盐缓冲盐水中 22 小时内释放了 91.7%。作为 INN 载体的分子瓶刷自组装颗粒可以有效地防止药物快速释放并延长释放时间，这是一种有前途的潜在临床应用候选药物。
