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大量的研究已经证明,紫杉醇口服吸收较差,容易引起过敏性反应。为了克服紫杉醇的不足,我们制备了一种新的纳米紫杉醇药物,它由甘露醇与人血清白蛋白包裹紫杉醇颗粒制成,其具有更好的水溶性和较低的毒性。为了进一步研究纳米紫杉醇口服给药后的吸收效果,我们利用Caco-2细胞模型对纳米紫杉醇的跨膜转运量进行了测定,3 h内,纳米紫杉醇在0.5～20μmol.L-1的浓度内的转运量呈线性状态。从膜的顶端到底端的表观渗透系数Papp为(20.9±2.1×10-6cm.s-1;N=3),米氏方程常数KM值为相对较高的14.00μmol.L-1,这些数据表明纳米紫杉醇具有更好的吸收效果。
A large number of studies have shown that paclitaxel oral absorption is poor, easily lead to allergic reactions. In order to overcome the deficiencies of paclitaxel, we prepared a new nano paclitaxel drug, which is made of mannitol and human serum albumin paclitaxel particles, which has better water solubility and lower toxicity. To further investigate the absorption effect of paclitaxel after oral administration, we measured the transmembrane transport of nanpaclitaxel using the Caco-2 cell model. Within 3 h, the nanosized paclitaxel concentration in the range of 0.5-20 μmol·L-1 Transport volume was linear. The apparent permeability coefficient (Papp) from the top to the bottom of the membrane was (20.9 ± 2.1 × 10-6cm · s-1; N = 3) and the Mk value was 14.00μmol.L-1. Show that nano paclitaxel has a better absorption effect.