Shim Woo Sun, Yoo Jae Sun, Bae You Han, Lee Doo Sung
Department of Polymer Science & Engineering, Sungkyunkwan University, Suwon, Gyunggi 440-746, Korea.
Biomacromolecules. 2005 Nov-Dec;6(6):2930-4. doi: 10.1021/bm050521k.
A novel pH and temperature sensitive block copolymer was prepared by adding pH sensitive moiety to temperature sensitive block copolymer. This block copolymer solution showed a reversible sol-gel transition by a small pH change in the range of pH 7.4-8.0 and also by the temperature change in the region of body temperature. The very precise molecular weight control of block copolymer and the prudential tuning of hydrophilic-hydrophobic balance were needed to control the phase diagram. This block copolymer solution forms a gel at 37 degrees C, pH 7.4 (human body). When the block copolymer solution is at room temperature and pH 8.0 as a sol state, both the temperature and pH change are needed for the gelation. This material can be employed as injectable carriers for hydrophobic drugs and proteins, etc. Gelation inside the needle can be prevented by an increase in the temperature during injection, because it does not change into the gel form with only increasing temperature. This material can be used for even a long guide catheter into the body. The block copolymer hydrogel which shows the sol-gel transition by the small pH change from pH 8.0 to pH 7.4 has merits in the delivery system for protein and cells which show cytotoxicity in acidic (below pH 6.5) or basic (above pH 8.5) conditions. This block copolymer system could be used as a template technology for injectable delivery systems.
通过向温度敏感型嵌段共聚物中添加pH敏感部分,制备了一种新型的pH和温度敏感型嵌段共聚物。该嵌段共聚物溶液在pH 7.4 - 8.0范围内通过微小的pH变化以及在体温区域内通过温度变化显示出可逆的溶胶-凝胶转变。为了控制相图,需要对嵌段共聚物进行非常精确的分子量控制以及对亲水-疏水平衡进行谨慎调节。这种嵌段共聚物溶液在37℃、pH 7.4(人体环境)下形成凝胶。当嵌段共聚物溶液在室温且pH 8.0处于溶胶状态时,凝胶化需要温度和pH都发生变化。这种材料可用作疏水性药物和蛋白质等的可注射载体。注射过程中温度升高可防止针内凝胶化,因为仅温度升高它不会转变为凝胶形式。这种材料甚至可用于插入体内的长导尿管。通过从pH 8.0到pH 7.4的微小pH变化显示出溶胶-凝胶转变的嵌段共聚物水凝胶,在蛋白质和细胞的递送系统中具有优势,这些蛋白质和细胞在酸性(pH低于6.5)或碱性(pH高于8.5)条件下具有细胞毒性。这种嵌段共聚物体系可作为可注射递送系统的模板技术。