几种药用高分子辅料的体内外毒性比较

发布时间：2018-05-14 02:43

本文选题：药用高分子辅料 + 细胞毒性　；参考：《海峡药学》2016年03期

【摘要】：目的通过细胞与动物实验,比较聚乙二醇1000维生素E琥珀酸酯(TPGS1000)、普朗尼克(F127)、单甲氧基聚乙二醇外消旋聚乳酸两嵌段共聚物(m PEG-PLA)及其三嵌段共聚物(PLA-PEG-PLA)、外消旋聚乳酸乙醇酸三嵌段共聚物(PLGA-PEG-PLGA)5种常用药用高分子辅料的体内外毒性,为选择安全有效的药用辅料提供实验依据。方法采用CCK-8法检测以上5种常用高分子药用辅料对人脐静脉内皮细胞HUVEC和人肝癌细胞Bel-7402的毒性;采用动物毒性试验方法初步观察5种辅料对小鼠的毒性反应。结果 TPGS在5种辅料中对细胞的毒性作用较强,其余4种辅料在1mg·m L~(-1)几无毒性表现,仅在5mg·m L~(-1)剂量下才表现出低毒。体内毒性实验中,TPGS的LD50约为500mg·kg~(-1),其他辅料在各剂量组小鼠均未出现明显毒性现象或死亡。结论体内外毒性试验结果提示:药用高分子辅料具有一定的毒性作用,将TPGS用作药用高分子辅料时,需特别考虑其用量,以确保新剂型的安全性;其他4种辅料在相同剂量下未表现出明显毒性,是比较安全的药用辅料。
[Abstract]:Objective through cell and animal experiments, Five kinds of polyethyleneglycol 1000 vitamin E succinic acid triblock copolymers (PLGA-PEG-PLAX, PLGA-PEG-PLGAA), Poly (ethylene glycol) triblock copolymers (PLGA-PEG-PLGAA), poly (ethylene glycol) (PEG-PEG-PLA), poly (glycolic acid) triblock copolymers (PLGA-PEG-PLGAA) were compared. In vivo and in vitro toxicity of polymer excipients for drug use, To provide experimental basis for the selection of safe and effective pharmaceutical excipients. Methods CCK-8 method was used to detect the toxicity of the above five kinds of macromolecule medical excipients to human umbilical vein endothelial cells (HUVEC) and human hepatoma cells (Bel-7402), and the animal toxicity test method was used to observe the toxicity of the five kinds of excipients to mice. Results the cytotoxicity of TPGS was stronger in the five kinds of excipients. The other four excipients showed little toxicity in 1mg mLL ~ (-1), but low toxicity only in the dosage of 5mg m L ~ (-1). In vivo toxicity test, the LD50 of LD50 was about 500mg KG-1, other excipients did not appear obvious toxic phenomenon or death in each dose group of mice. Conclusion the results of in vivo and in vitro toxicity tests suggest that medicinal polymer excipients have certain toxic effects, and the dosage of TPGS should be taken into account in order to ensure the safety of the new dosage form. The other four kinds of excipients showed no obvious toxicity at the same dose, and were relatively safe for medicinal excipients.
【作者单位】：福建中医药大学药学院;福建卫生职业技术学院药学系;
【基金】：国家卫计委科研项目(WKJ-FJ-06) 福建省中医药科研课题(wzzy201307) 福建卫生职业技术学院科研启动资助项目(2013-1-1)
【分类号】：R96

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