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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。
Objective To study the potential absorption characteristics of hydroxycamptothecin nanosuspensions in the small intestine. Methods Caco-2 cell model was used to study the cellular uptake and transmembrane transport of hydroxycamptothecin nanosuspension with different mass concentrations. Results Hydroxycamptothecin nanosuspension showed good absorption characteristics in Caco-2 cell model, and cell uptake increased with the increase of preparation concentration, such as 50, 100 and 200 mg.L-13 The cellular protein uptake of the test preparations was 11.684 6,26.452 4 and 30.903 9 mg.g-1, respectively, and the permeation coefficient Papp was 100 mg.L-1. AP → BL was 27.8 ± 1.37 × 10 -7) cm.s-1. Conclusion The experimental results show that the nano-suspension can effectively increase the amount of hydroxycamptothecin and transmembrane transport rate. Therefore, nanosuspensions may help improve the oral bioavailability of hydroxycamptothecin.