甘露聚糖修饰的靶向纳米脂质体的抗肿瘤作用实验研究

目的研究甘露聚糖修饰的靶向纳米脂质体的抗肿瘤作用。方法用胆固醇氯甲酸醋和N，N-二甲基乙二胺反应生成313N-（N’，N’-二甲基氨基乙烷）-氨基甲酰]胆固醇（DC—chol），以DC—chol、二棕榈磷脂酰基乙醇胺（DoPE）和N-2-（胆固醇氧羰基氨基）乙基]用氨酰甲基化革露聚糖（chol—AECM—mannan）为原料合成甘露聚糖修饰的靶向纳米脂质体，检测脂质体粒径大小。应用C57小鼠制备移植性肺癌模型，静脉给予各种纳米脂质体（实验纳米脂质体，无革露聚糖修饰的包裹有EGFR的纳米脂质体、空纳米脂质体）及对照EGFR，观察小鼠的一般情况及肿瘤生长情况；行ELISA和Western Blotting检测小鼠血清中抗体漓度差别。结果脂质体粒径大小为132．6nm。ELISA和Western Blotting检测均显示实验组小鼠血清有抗体产生而且抗体漓度远大于其他对照组。实验组肿瘤体积明显小于对照组（EGFR及空白脂质体组，P〈0．05）。结论研究结果表明实验组小鼠肿瘤生长受到抑制，甘露聚糖修饰的靶向纳米脂质体对小鼠肺癌有一定疗效。

Experimental Study of Anti-cancer Effect of Mannan-modified Targeted Nanoliposome on Mice

OBJECTIVE: To test the anti-cancer effect of mannan-modified targeted nanoliposome on mice. METHODS: The 3betaN-(N',N'-dimethylaminoethane) -carbamoyl] cholesterol (DC-chol) was synthesized by the chemical reaction of cholesteryl chloroformate and N, N-dimethylethylendiamine. The DC-chol was then mixed with dioleoylphosphatidylethanolamine (DOPE) and chol-AECM-mannan to produce the sonicated mannan-modified targeted nanoliposome. The size of the nanoliposome was measured by zetasizer. Nanoliposome or purified EGFR (as control) was injected to the C57 mice with implanted lung cancers intravenously. The growth of tumors was observed, followed by ELISA and Western tests of serum antibodies. RESULTS: The liposome nanoparticle had a size of 132 nm. The experimental groups had significant higher levels of blood serum antibodies than the controls. The experimental groups also had less volumes of tumors than the controls (P<0.05). CONCLUSION: The growth of tumor has been inhibited by mannan-modified targeted nanoliposome. The mannan-modified targeted nanoliposome has anti-cancer effect on mice.