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目的 :观察颈淋巴结靶向性葫芦素BE聚乳酸纳米微粒 (CuBE_PLA_NP)冻干针剂的急性毒性作用和对局部组织的刺激反应 ,为动物实验和临床实验提供依据。方法 :用不同剂量的CuBE_PLA_NP冻干针剂和葫芦素BE(CuBE)行小鼠皮下和尾静脉注射 ,观察小鼠用药后的毒副反应 ,并计算半数致死量 (LD50 ) ;用CuBE_PLA_NP冻干针剂和CuBE行兔股四头肌注射 ,观察药物对局部组织的刺激性。结果 :CuBE_PLA_NP冻干针剂皮下和静脉注射的LD50 值分别为 16 74mg/kg± 1 83mg/kg和 5 6 0mg/kg± 0 83mg/kg,CuBE皮下和静脉注射的LD50 值分别为 8 6 3mg/kg±1 0 0mg/kg和 2 5 0mg/kg± 0 30mg/kg。CuBE_PLA_NP冻干针剂局部肌肉注射的反应数均为 0级 ,CuBE的反应数为0~ 1级。结论 :CuBE_PLA_NP冻干针剂对机体的毒副作用和局部刺激性小于CuBE ,CuBE_PLA_NP和CuBE都可用作局部注射
Objective : To observe the acute toxicity and stimulating response to local tissues of cervical lyphile-targeted cucurbitacin BE poly(lactic acid nanoparticles) (CuBE_PLA_NP) lyophilized injections for animal experiments and clinical experiments. METHODS: Different doses of CuBE_PLA_NP lyophilized needles and cucurbitacin BE (CuBE) were injected subcutaneously and in tail vein of mice. The toxicity of mice after administration was observed, and the median lethal dose (LD50) was calculated; and CuBE_PLA_NP freeze-dried injection was used. CuBE was injected into the quadriceps muscle of rabbits to observe the local irritation of the drug. Results: The LD50 values of subcutaneous and intravenous injections of CuBE_PLA_NP lyophilized injections were 16 74 mg/kg ± 183 mg/kg and 560 mg/kg ± 0 83 mg/kg, respectively. The LD50 values of CuBE subcutaneous and intravenous injections were 864 mg/kg, respectively. Kg ± 1000 mg/kg and 250 mg/kg ± 30 mg/kg. The reactions of CuBE_PLA_NP lyophilized injection with local intramuscular injection were all grade 0, and the response of CuBE was grade 0–1. Conclusion : CuBE_PLA_NP lyophilized injections have fewer toxic side effects and local irritation than CuBE. CuBE_PLA_NP and CuBE can be used as local injections.