Department of Pharmacology, School of Medicine, Shandong University, Jinan, China.
Colloids Surf B Biointerfaces. 2011 Oct 15;87(2):319-25. doi: 10.1016/j.colsurfb.2011.05.037. Epub 2011 May 27.
The aim of the present study was to evaluate both the in vitro and in vivo antitumor activity of an oridonin nanosuspension (ORI-N) relative to efficacy of bulk oridonin delivery.
ORI-N with a particle size of 897.2±14.2 nm and a zeta potential of -21.8±0.8 mV was prepared by the high-pressure homogenization (HPH) technique. The in vitro cytotoxicity of ORI-N against SMMC-7721 cells was evaluated by MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay, the effects of ORI-N on cell cycle and cell apoptosis was analyzed by flow cytometry; the in vivo anti-tumor activity was observed in H22 tumor bearing mice.
ORI-N effectively inhibited the proliferation of SMMC-7721 cells. Flow cytometric analysis demonstrated that ORI-N arrested SMMC-7721 cells in the G2/M cycle, and furthermore, that ORI-N induced a higher apoptotic rate than the bulk ORI solution. In vivo studies ORI-N also showed higher antitumor efficacy as measured by reduced tumor volume and tumor weight, as well as lower toxicity in H22 solid tumor bearing mice compared to free ORI at the same concentration.
These results suggest that the delivery of ORI-N as a nanosuspension is a promising approach for treating tumors.
本研究旨在评估冬凌草甲素纳米混悬剂（ORI-N）相对于体相冬凌草甲素给药的体内外抗肿瘤活性。
采用高压均质（HPH）技术制备粒径为 897.2±14.2nm、Zeta 电位为-21.8±0.8mV 的 ORI-N。采用 MTT[3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐]法评价 ORI-N 对 SMMC-7721 细胞的体外细胞毒性，采用流式细胞术分析 ORI-N 对细胞周期和细胞凋亡的影响；在 H22 荷瘤小鼠中观察 ORI-N 的体内抗肿瘤活性。
ORI-N 能有效抑制 SMMC-7721 细胞的增殖。流式细胞术分析表明，ORI-N 将 SMMC-7721 细胞阻滞在 G2/M 期，并且诱导的凋亡率高于体相 ORI 溶液。体内研究还表明，与相同浓度的游离 ORI 相比，ORI-N 纳米混悬剂在 H22 荷瘤小鼠中具有更高的抗肿瘤疗效，表现为肿瘤体积和重量减小，毒性降低。
这些结果表明，ORI-N 纳米混悬剂的递送是治疗肿瘤的一种有前途的方法。
