紫杉醇-两亲性壳聚糖胶束大鼠药代动力学和在体肠吸收
Pharmacokinetics and in situ absorption in rat intestine of paclitaxel-loaded amphiphilic chitosan micelle
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摘要: 以紫杉醇（paclitaxel,PTX）注射剂Taxol为对照，通过大鼠药代动力学及在体肠吸收实验考察N-辛基-O，N-羧甲基壳聚糖（OCC）胶束作为PTX口服给药系统的可行性。结果表明，与Taxol相比，PTX-OCC胶束经口给药在大鼠体内的cmax、AUC均显著提高(P<0.05)，相对生物利用度为331.4%；PTX-OCC胶束在各个肠段吸收均显著高于Taxol(P<0.05)，且十二指肠吸收略优于其他肠段，结肠、空肠和回肠吸收相近，说明OCC胶束具有显著的促吸收效果，作为难溶性药物口服递送载体具有优良的应用前景。Abstract: The aim of this study was to investigate the potential feasibility of the N-octyl-O,N-carboxymethyl chitosan (OCC) micelles as oral administration carriers for paclitaxel (PTX) by pharmacokinetics and in situ absorption in rat intestine using Taxol as control.After oral administration of PTX-OCC micelles,the area under the plasma concentration-time curve (AUC) and the maximum concentration (cmax) were significantly larger than those of Taxol (P<0.05).Relative bioavailability for PTX-OCC micelles was 331.4% of that of Taxol.The absorption of PTX-OCC at different segments of intestine was significantly higher than those of Taxol(P<0.05).The apparent absorption rate (Ka)and the effective permeation coefficient (Peff) at the duodenum were a little higher than those of jejunum,ileum and colon (P>0.05).In conclusion，OCC might be a promising carrier for oral administration of poorly water-soluble drugs.
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Keywords:
- chitosan /
- self-assembled polymeric micelle /
- paclitaxel /
- pharmacokinetics /
- intestinal absorption
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