大鼠在体肠回流法研究环孢素纳米脂质体的吸收行为

Absorption behavior of cyclosporin nanoliposome by in situ circulation method in rats

目的 :研究环孢素纳米脂质体在大鼠小肠的吸收行为。方法 :利用旋转薄膜 超声法制备环孢素纳米脂质体。采用大鼠在体回流法研究脂质体在大鼠小肠的吸收行为。结果 :当脂质体中药物浓度从 1g·L- 1逐渐增至 2 .4 g·L- 1时 ,累积吸收量从(0 .0 2 5±s 0 .0 2 4 )mg·cm- 2 增至 (0 .0 6 7± 0 .0 0 7)mg·cm- 2 ,但当浓度继续增至 7.5 g·L- 1时 ,累积吸收量缓慢增至 (0 .0 85± 0 .0 11)mg·cm- 2 ,呈现饱和现象。使用载体竞争剂和降低Na+浓度 ,对累积吸收量没有显著影响 (P >0 .0 5 ) ;应用能量抑制剂 (二硝基苯酚 )和P 糖蛋白抑制剂 (维拉帕米 )均使累积吸收量从 (0 .0 90± 0 .0 2 0 )mg·cm- 2 增至 (0 .15± 0 .0 3)mg·cm- 2 ,有显著促进作用 (P <0 .0 1)。结论

AIM: To investigate the absoption behavior of cyclosporin nanoliposome in the small intesteine of rats. METHODS: Cyclosporin nanoliposome was prepared by the rotary evaporation method, and further with sonication. In situ circulation method was utilized. RESULTS: As the concentration of cyclosporin increased from 1 g·L -1 to 2.4 g·L -1 , the accumulated absorption increased correspondingly from (0.025±0.024) mg·cm -2 to ( 0.067 ±0.007) mg·cm -2 . But when the concentration increased to 7.5 g·L -1 , the absorption amount increased steadily to (0.085±0.011) mg·cm -2 , which showed a saturated absorption. Neither carrier competitor nor decreasing the concentration of Na + had any influence on absorption ( P >0.05). Both the energy inhibitor(dinitrophenol) and P glycoprotein inhibitor(verapamil) increased the absorption, significantly from (0.090±0.020) mg·cm -2 to (0.15± 0.03 ) mg·cm -2 ( P <0.01). CONCLUSION: The absorption of cyclosporin nanoliposome in the small intestine of rats may be transported through phagcytosis of lymph system.