Research Institute of Drug Development, Chonnam National University, Gwangju, Korea.
Arch Pharm Res. 2010 May;33(5):761-7. doi: 10.1007/s12272-010-0516-7. Epub 2010 May 29.
For a new anticancer drug carrier, we synthesized 4 compositions of amphiphilic stearic acidconjugated pullulan (SAP) and characterized them with FT-IR spectroscopy. Crystalline changes were verified by x-ray diffraction patterns before and after synthesis of the SAP conjugate. SAP nanoparticles were prepared by a diafiltration method, and the fluorescence spectroscopy using pyrene showed particle self-assembly in water. SAP nanoparticles were spherical in TEM photos, and particle size ranged between 200 approximately 500 nm in photon correlation spectroscopy. Release of all-trans-retinoic acid from the SAP nanoparticles was maintained over 5 weeks. For further study in vivo, we tested the cytotoxicity of SAP nanoparticles using an MTT assay, and cytotoxicity was augmented as the molar mass of stearic acid increased in human liver carcinoma HepG2 cells. Therefore, SAP nanoparticles might be a promising longterm delivery carrier for hydrophobic therapeutic molecules with the appropriate composition.
为了开发一种新型的抗癌药物载体，我们合成了 4 种两亲性硬脂酸接枝普鲁兰（SAP），并用傅里叶变换红外光谱（FT-IR）对其进行了表征。通过合成前后 SAP 缀合物的 X 射线衍射图谱验证了晶体变化。通过渗滤法制备 SAP 纳米粒子，并使用芘进行荧光光谱分析表明，SAP 纳米粒子在水中自组装。TEM 照片显示 SAP 纳米粒子呈球形，光子相关光谱法测定的粒径在 200 到 500nm 之间。全反式维甲酸（all-trans-retinoic acid）从 SAP 纳米粒子中的释放可维持 5 周以上。为了进一步进行体内研究，我们使用 MTT 测定法测试了 SAP 纳米粒子的细胞毒性，结果表明，在人肝癌 HepG2 细胞中，随着硬脂酸摩尔质量的增加，SAP 纳米粒子的细胞毒性增强。因此，SAP 纳米粒子可能是一种有前途的、适合于疏水性治疗分子的长效递药载体。
