OBJECTIVE: To study absorption mechanism and anti-tumor effect in mice of Norcantharidin loaded N-galactosylat-ed chitosan nanoparticles (NCTD-GC-NPs). METHODS: Using apparent coefficient as index, effects of NCTD-GC-NPs (80 μg·mL-1) combined with cyclosporin A (CyA, 50 μmol·L-1), sodium deoxycholate (SDCh, 100 mmol·L-1), NaN3 (25 mmol·L-1) or oxo-phenylarsine (25 mmol·L-1) on Caco-2 cell transport were investigated; after the vaccination of H22, mice were randomly divided into blank group, control group (NCTD raw material 2 mg·kg-1), NCTD-GC-NPs high-dose, medium-dose and low-dose groups (0.5, 2, 4 mg·kg-1) with each group of 10 mice. Those groups were given medicine via i.g. once a day for consecutive 8 days. The body weight and anti-tumor rate were investigated during this experiment. RESULTS: CyA, SDCh and NaN3 could improved the transportation of NCTD-GC-NPs in Caco-2 cells significantly (P<0.05 or P<0.01), while oxophenylarsine showed no obvious effect. The body weight of mice had no significant change. Compared with control group, the anti-tumor rate of NCTD-GC-NPs of medium-dose and high-dose groups were enhanced significantly (P<0.05 or P<0.01). CONCLUSION: NCTD-GC-NPs may pass through intestinal epithelial cells primarily by active transport, which could inhibit the growth of hepatic carcinoma cell H22.%目的:研究去甲基斑蝥素N-乳糖酰壳聚糖纳米粒(NCTD-GC-NPs)的吸收机制和小鼠抑瘤作用.方法:以表观透过系数为指标,考察NCTD-GC-NPs(80 μg· mL-1)及其分别与环孢素A(50 μmol· L-1)、去氧胆酸钠( 100 mmol· L-1)、叠氮化钠(25 mmol·L-1)、氧化苯胂(25 mmol·L-1)联用后对结肠癌Caco-2细胞转运的影响；将接种肝癌细胞H22后的小鼠随机分为空白组、对照组(NCTD原料药2 mg·kg-1)和NCTD-GC-NPs低、中、高剂量组(0.5、2、4 mg·kg-1),每组10只,每日灌胃给药1次,连续给药8d,考察各组小鼠体重和抑瘤率.结果:环孢素A、去氧胆酸钠和叠氮化钠均能明显促进NCTD-GC-NPs在Caco-2细胞的转运(P＜0.05或P＜0.01),氧化苯胂对转运无明显影响；各组小鼠体重无明显变化；与对照组比较,NCTD-GC-NPs中、高剂量组的抑瘤率明显增强(P＜0.05或P＜0.01).结论:NCTD-GC-NPs主要通过主动转运穿过小肠上皮细胞,能明显抑制肝癌肿瘤细胞H22的生长.
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