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去甲斑蝥素(norcantharidin, NCTD)是斑蝥素的去甲基化衍生物,与斑蝥素相比能降低对肾脏的毒副作用和泌尿系统的刺激性。目前,NCTD临床应用形式以注射和口服为主,在肿瘤疾病治疗上有一定效果,如能抑制DNA复制,促进肿瘤细胞死亡,对多种肿瘤细胞具有细胞毒性且有一定升高白细胞的作用,具有显著的保护肝细胞的作用[1-3]。现代临床主要用于治疗肝癌、肺癌、乳腺癌、膀胱癌、胃癌和食管癌,但其治疗窗窄,LD50值低、毒性大等缺陷使其临床应用受到了限制[4]。近年来,NCTD滴丸和软胶囊两种剂型也表现出稳定性好、生物利用度高等优点,研究者正利用新型制剂的靶向性、缓控释等作用特点,增强靶向给药性,减少药物在肾脏分布和对泌尿系统的刺激作用,使其在肿瘤疾病中发挥更显著的疗效。
Research progress in new formulations of norcantharidin
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摘要:
目的 综述去甲斑蝥素新型制剂研究进展。 方法 通过查阅近年来有关去甲斑蝥素新型制剂的中外文献,对其研究进展进行归纳总结与分析。 结果 经过对微球、纳米粒、脂质体和微乳等载药系统包载去甲斑蝥素的情况进行分析,结果表明去甲斑蝥素新型制剂是极具开发潜力的新型制剂。 结论 去甲斑蝥素是一种优良的抗肿瘤药物,但传统的注射剂和片剂在临床应用上有很大的毒副作用。根据目前研究结果显示,将其制备为新型制剂可以增强靶向性,减小对肾脏和泌尿系统的毒副作用,更好地发挥药效。因此,将去甲斑蝥素制成新型制剂具有良好的发展前景。 Abstract:Objective To review the research progress in new formulations of norcantharidin. Methods The foreign and domestic literature search in the new formulations of norcantharidin was conducted. The research and development of norcantharidin formulations were summarized and commented. Results The drug delivery systems, such as microspheres, nanoparticles, liposomes, and microemulsions, have great development potential as the new formulations for norcantharidin. Conclusion Norcantharidin is an excellent anti-tumor drug. The traditional injections and tablets have serious side effects in clinical application. The new formulations reduced the renal and urinary toxicity and side effects. Those formulations provided better therapeutic effects as target medication. Therefore, the new norcantharidin formulations have great development prospects. -
Key words:
- norcantharidin /
- microspheres /
- nanoparticles /
- liposomes /
- microemulsions
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