Sun Tao-Li, Wang Bin, Peng Yan, Ni Jing-Man
School of Pharmacy, Lanzhou University, Lanzhou 730000, China.
Yao Xue Xue Bao. 2013 Jan;48(1):149-54.
The purpose of this study is to investigate the intracellular transporters effect and the cytotoxicity of carboxyl nanodiamond (CND) - podophyllotoxin (PPT). Nanodiamond (ND) was treated with mixed carboxylic acid and finally got 64 nm CND by centrifugation, and then it was reacted with PPT to form CND-PPT. UV spectrophotometry was used to calculate the content of PPT in CND-PPT, the particle size distribution and zeta potential were measured by Dynamic laser scattering instrument. CND, PPT, CND-PPT and CND + PPT (physical mixture of CND and PPT) were characterized by Fourier transform infrared spectroscopy, at the same time, thermal analysis and element analysis were used to estimate the content of the PPT in CND-PPT. The affect of CND, PPT, CND-PPT on HeLa cell was measured with MTT assay. The results showed that content of PPT combined with CND accounted for about 10%. MTT assay showed that CND has low cytotoxicity and CND-PPT can increase the water soluble of PPT. As a conclusion, CND as a hydrophilic pharmaceutical carrier combined with PPT is able to increase the water solubility of PPT, at low concentration, CND-PPT can enhance the antitumor activity in comparison with PPT, so CND can be used as a potential anticancer drug carrier.
本研究旨在探讨羧基纳米金刚石（CND）-鬼臼毒素（PPT）的细胞内转运作用及细胞毒性。纳米金刚石（ND）用混合羧酸处理，通过离心最终得到64 nm的CND，然后使其与PPT反应形成CND-PPT。采用紫外分光光度法计算CND-PPT中PPT的含量，用动态激光散射仪测量粒径分布和zeta电位。通过傅里叶变换红外光谱对CND、PPT、CND-PPT和CND + PPT（CND与PPT的物理混合物）进行表征，同时采用热分析和元素分析来估算CND-PPT中PPT的含量。用MTT法检测CND、PPT、CND-PPT对HeLa细胞的影响。结果表明，与CND结合的PPT含量约为10%。MTT法显示CND具有低细胞毒性，且CND-PPT能提高PPT的水溶性。结论是，CND作为亲水性药物载体与PPT结合能够提高PPT的水溶性，在低浓度下，与PPT相比，CND-PPT可增强抗肿瘤活性，因此CND可作为一种潜在的抗癌药物载体。
