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目的:制备蛇床子素-Eudragit S100-pH敏感型纳米粒(Ost-S100-NP),并考察Ost-S100-NP体内和体外的抗肿瘤活性。方法:以乳化-溶剂扩散法制备Ost-S100-NP胶体溶液,体外采用MTT法考察Ost和Ost-S100-NP对宫颈癌细胞Hela-3的抑制作用;体内Ost对小鼠宫颈癌U14实体瘤的抗肿瘤试验采用常规的抗肿瘤试验方法,考察不同给药浓度、不同剂型对小鼠体质重、肿瘤生长和胸腺、脾及肝等脏器质量变化的影响。结果:Ost体外对Hela-3细胞的半数抑制浓度IC50分别为:61.25,56.87,48.46μg/mL;Ost-S100-NP的IC50则分别为46.57,40.23,37.46μg/mL;体内Ost及其Ost-S100-NP制剂对荷瘤小鼠的实体瘤抑制率最高可达40%,各给药组与空白对照组比较,差异有统计学意义(P<0.01)。结论:Ost-S100-NP体外和体内均有明显的抗肿瘤活性,且在治疗剂量下未出现毒性反应,有望开发成1种高效、低毒的Ost-S100-NP制剂。
OBJECTIVE: To prepare Ostragas S100-pH-sensitive nanoparticles (Ost-S100-NP) and investigate the antitumor activity of Ost-S100-NP in vitro and in vivo. Methods: Ost-S100-NP colloidal solution was prepared by emulsion-solvent diffusion method. The inhibitory effect of Ost and Ost-S100-NP on cervical cancer cell Hela-3 was investigated by MTT method in vitro. Anti-tumor test using conventional anti-tumor test methods to study the different concentrations, different formulations of mice weight, tumor growth and thymus, spleen and liver and other organ quality changes. Results: The IC50 values of Ost against Hela-3 cells in vitro were 61.25, 56.87 and 48.46 μg / mL, respectively. The IC50 values of Ost-S100-NP were 46.57, 40.23 and 37.46 μg / mL, respectively. The inhibition rate of S100-NP to solid tumor in tumor-bearing mice was up to 40%, and the difference was statistically significant (P <0.01) between each administration group and blank control group. Conclusion: Ost-S100-NP has obvious antitumor activity in vitro and in vivo, and no toxic reaction occurs at the therapeutic dose. It is expected to be an Ost-S100-NP preparation with high efficiency and low toxicity.