华西口腔医学杂志

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颈淋巴结靶向葫芦素BE聚乳酸纳米微粒的急性毒性和局部刺激实验研究

杨凯,温玉明,李龙江,王昌美,王晓毅   

  1. 400016 重庆医科大学附属第一医院口腔颌面外科 (杨 凯),四川大学华西口腔医院(温玉明,李龙江,王昌美,王晓毅)
  • 收稿日期:2001-12-25 修回日期:2001-12-25 出版日期:2001-12-20 发布日期:2001-12-20
  • 基金资助:
    本课题为卫生部科学基金资助项目(编号98-1-221)

Acute Toxicity and Local Stimulate Test of CucurbitacinBE Polylactic Acid Nano-particles of Targeting Cervical Lymph Nodes

Yang Kai, Wen Yuming, Li Longjiang,et al   

  1. Yang Kai Department of Stomatology, the First Affiliated Hospital, Chongqing Medical University Wen Yuming, Li Longjiang, Wang Changmei,et al College of Stomatology, West China University of MedicalSicences
  • Received:2001-12-25 Revised:2001-12-25 Online:2001-12-20 Published:2001-12-20

摘要:

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16.74 mg/kg±1.83 mg/kg和5.60 mg/kg±0.83 mg/kg,CuBE皮下和静脉注射的LD50值分别为8.63 mg/kg±1.00 mg/kg和2.50 mg/kg±0.30 mg/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。

关键词: 葫芦素BE, 聚乳酸, 纳米微粒, 颈淋巴结转移灶, 靶向化疗, 副作用

Abstract:

Objective:The aim of this experiment was to study acute toxicity and local stimulation of cucurbitacinBE poly-lactic acid nano-particles (CuBE-PLA-NP) fortargeting cervical lymph node.Methods:Various doses of CuBE-PLA-NP lyophilization injec- tion and cucurbitacinBE (CuBE) were hypodermically or veno-injected into the mice, and then the drug toxicity and side effects were observed; 50% lethal dose (LD50) was counted. CuBE-PLA-NP lyophilization injection and CuBEwere also injected into the quadriceps femoralis muscle of rabbits to observe the local stimulate responses of drugs.Results:The fifty percent lethal doses of subcutaneous and venous CuBE-PLA-NP in mice were 16174 mg/kg?1183 mg/kg and 5160 mg/kg?0183 mg/kg respectively, thatwere higher than those of CuBEwhich were 8163 mg/kg?1100 mg/kg and 2150 mg/kg?0130 mg/kg respectively. Local stimulate response in rabbit quadricepsfemoralismuscle afterCuBE-PLA-NP and CuBEinjected are 0 grade and 011 grade respec- tively.Conclusion:The acute toxicity of CuBE-PLA-NP is lower than thatof CuBE. Both CuBE-PLA-NP and CuBE are adequate for local injection, but the local stimulation of CuBE-PLA-NP is smaller than that of CuBE.

Key words: cucurbitacinBE, poly-lactic acid, nano-particles, targeted chemotherapy, side effects