羟基喜树碱纳米混悬剂在Caco-2细胞模型中的吸收特性

目的研究羟基喜树碱纳米混悬剂在小肠内潜在的吸收特性。方法采用Caco-2细胞模型研究不同质量浓度的羟基喜树碱纳米混悬剂的细胞摄取与跨膜转运。结果羟基喜树碱纳米混悬剂在Caco-2细胞模型上显示出很好的吸收特性,且细胞摄取量随着制剂质量浓度的增加而增加,如:50、100和200 mg.L-13个试验质量浓度制剂的细胞蛋白摄取量分别为11.684 6、26.452 4和30.903 9 mg.g-1,试验质量浓度为100 mg.L-1制剂的细胞转运渗透系数Papp,AP→BL为(27.8±1.37×10-7)cm.s-1。结论试验结果证明,纳米混悬剂能有效地增加羟基喜树碱的细胞摄取量和跨膜转运速率。因此,纳米混悬剂可能有助于提高羟基喜树碱的口服生物利用度。

Absorption of hydroxycamptothecin nanosuspension across Caco-2 cells monolayer

Objective To study the potential absorption properties of hydroxycamptothecin (HCPT) nanosuspension in the small bowel. Method The uptake and the transport across cells for different concentration of HCPT nanosuspension were performed with Caco-2 cells. Results The test data indicated that HCPT nanosuspension had a good absorption characteristic in the Caco-2 cells. The results showed the uptake of 50 mg·L^-1, 100 mg·L^-1, 200 mg·L^-1 HCPT nanosuspension were 11.684 6 mg·g^-1 protein, 26.452 4 mg·g^-1 protein, 30.903 9 mg·g^-1 protein，respectively. The membrane permeability coefficient of 100 mg·L^-1 HCPT nanosuspension was (27.8±1.37×10^-7) cm·s^-1. Conclusion The results demonstrated that the uptake and the transport ratio increased with increasing concentration of HCPT nanosuspension. Therefore, nanosuspension could effectively increase the uptake and transport rate of HCPT.