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采用融熔法制备了氨甲喋吟(MTX)多相脂质体,并进行了抑瘤活性、小鼠急性毒性、家兔亚急性毒性和安全性实验。结果表明多相脂质体剂型显著提高了 MTX 对小鼠 EC 和 L615瘤株的抑瘤活性。急性毒性实验结果表明 MTX 多相脂质体和 MTX 水溶液的 ivLD_(50)值无显著性差异。亚急性毒性实验表明 MTX 多相脂质体大剂量给药时可出现肝细胞变性坏死。安全性实验未见异常反应。
The methotrexate (MTX) multiphasic liposomes were prepared by melting method. The antitumor activity, acute toxicity in mice, subacute toxicity and safety of rabbits were also tested. The results showed that the multiphasic liposomal formulations significantly increased the inhibitory activity of MTX against mouse EC and L615 tumor strains. The results of the acute toxicity test showed that there was no significant difference in the ivLD_ (50) value between MTX multiphase liposome and MTX water solution. Subacute toxicity experiments showed that MTX multiphasic liposomes may appear when hepatocyte degeneration and necrosis at high doses. No abnormal reaction safety experiment.