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目的研究鹰嘴豆芽素A(BCA)及其聚乙二醇化纳米脂质载体(PEG-BCA-NLC)的细胞吸收转运机制。方法用Caco-2细胞模型研究BCA及PEG-BCA-NLC的摄取、转运及其影响因素;用高效液相色谱法检测BCA浓度,计算其表观通透系数(Papp)。结果 Caco-2细胞对BCA及PEG-BCANLC的吸收符合被动扩散过程,但相同时间下BCA的摄取量较PEG-BCA-NLC高;加入维拉帕米可有效提高Caco-2细胞对PEG-BCA-NLC的吸收转运,Papp(肠腔侧→基底层,AP→BL)增大,而Papp(BL→AP)变小,但转运量仍较BCA溶液组低。结论 PEG-BCA-NLC在Caco-2细胞模型中的吸收转运主要是被动扩散方式,PEG-BCA-NLC不一定能显著提高药物在小肠的吸收。
OBJECTIVE To study the cellular uptake and transport mechanism of biochanin A (BCA) and its pegylated nanosized lipid carrier (PEG-BCA-NLC). Methods Caco-2 cell model was used to study the uptake and transport of BCA and PEG-BCA-NLC and their influencing factors. The BCA concentration was measured by HPLC, and the apparent permeability coefficient (Papp) was calculated. Results The uptake of BCA and PEG-BCANLC in Caco-2 cells was in accordance with the passive diffusion process, but the uptake of BCA was higher than that of PEG-BCA-NLC at the same time. The addition of verapamil effectively increased the uptake of PEG-BCA - Papp (intestinal compartment → basal layer, AP → BL) increased while Papp (BL → AP) decreased, but the transport volume was still lower than that of BCA solution. Conclusion The absorption and transport of PEG-BCA-NLC in Caco-2 cell model are mainly passive diffusion. PEG-BCA-NLC does not necessarily increase the absorption of drugs in the small intestine.