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Antitumor activity of mitoxantrone-nanosphereagain liver tumor

机译:米托蒽醌-纳米球再次对肝肿瘤的抗肿瘤活性

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To comparing antitumor activity against experimental liver tumor H_(22) in mice of mitoxantrone-polybutycyanoacrylate-nonosphere (DHAQ-PBCA-NS), a liver targeting drug delivery system and mitoxantrone(DHAQ). Methods Drugs were given iv on the 1st, 5th, 9th day after planting tumor respectively. Weight of tumor in mouse was measured and rate of tumor inhibition (RTI) was studied. And the result were compared with those of mitoxantrone (DHAQ). Time-effect relationship was also observed when the same doses of drugs were administrated. Results There was relationship of dose-effect for DHAQ and DHAQ-PBCA-NS and ED_(50) of DHAQ and DHAQ-PBCA-NS was 1.04mg/kg and 0.34mg/kg respectively. The LD_(50) of DHAQ and DHAQ-PBCA-NS iv in mice with the same administration schedule was 3.670mg/kg and 4.225mg/kg respectively. Therefore, the therapeutic index of both drugs was known, that was 3.53 for DHAQ and 12.43 for DHAQ-PBCA-NS. For two drugs, the earlier the administration, the higher rate of tumor inhibition (RTI). But the RTI of DHAQ-PBCA-NS was higher than that of DHAQ if the drugs were give at the same time. Conclusion The results showed that antitumor activity of DHAQ-PBCA-NS was much higher than that of DHAQ, and the acute toxicity of DHAQ-PBCA-NS was lower. DHAQ-PBCA-NS showed liver targeting.
机译:为了比较对米托蒽醌-聚丁酸氰基丙烯酸酯-诺诺球(DHAQ-PBCA-NS),肝靶向药物递送系统和米托蒽醌(DHAQ)小鼠的实验性肝肿瘤H_(22)的抗肿瘤活性。方法种植肿瘤后第1、5、9天分别静脉给药。测量小鼠的肿瘤重量,并研究肿瘤抑制率(RTI)。并将结果与​​米托蒽醌(DHAQ)进行比较。当施用相同剂量的药物时,也观察到时间效应关系。结果DHAQ和DHAQ-PBCA-NS存在剂量效应关系,DHAQ和DHAQ-PBCA-NS的ED_(50)分别为1.04mg / kg和0.34mg / kg。 DHAQ和DHAQ-PBCA-NS iv在相同给药方案下的小鼠的LD_(50)分别为3.670mg / kg和4.225mg / kg。因此,已知两种药物的治疗指数,DHAQ为3.53,DHAQ-PBCA-NS为12.43。对于两种药物,越早给药,肿瘤抑制率(RTI)越高。但是,如果同时给予药物,DHAQ-PBCA-NS的RTI高于DHAQ。结论:DHAQ-PBCA-NS的抗肿瘤活性明显高于DHAQ,而DHAQ-PBCA-NS的急性毒性较低。 DHAQ-PBCA-NS显示出肝靶向性。

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