摘要
目的对壳聚糖修饰的托氟啶纳米脂质体的体外释放行为进行研究。方法以托氟啶溶液为对照,采用动态膜透析法考察壳聚糖修饰托氟啶纳米脂质体(TFu-SLNs)在磷酸盐缓冲液(pH=7.4)、人工胃液(pH=1.2)、肠液(pH=6.8)以及人工胃液转肠液中的体外释药情况并测定其方法回收率。结果托氟啶溶液在磷酸缓冲液、人工胃液、人工肠液释放均符合一级速率方程,方程分别为A=37602C+160.48(r=0.9999)、A=39488C+1915.3(r=0.9998)、A=38790C-194.11(r=0.9993)。在人工胃液中壳聚糖修饰TFu-SLNs符合Ritger-Peppas方程,lnQ=0.3984lnt+3.1352(r=0.9796);在人工肠液及人工胃液转肠液中中壳聚糖修饰TFu-SLNs均符合Weibull方程,方程分别为lnQ=0.3852lnt-1.32586(r=0.9645)、lnQ=0.4126lnt-1.2702(r=0.9746)。结论壳聚糖修饰的TFu-SLNs可缓慢释放药物,且其释放药物的机制以药物扩散为主。
Objective To study the in vitro drug release of chitosan modified N3-O-toluyl-flulorouracil（ TFu） Solid Lipid Nanoparticles（ SLNs）. Methods The released kinetics of chitosan modified TFu- SLNs in vitro of different media, such as the phosphate buffer solution（ pH = 7. 4）, artificial gastric juice（ pH = 1. 2）, artificial intestinal juice（ pH = 6. 8）, and artificial gastric juice followed by aritifical intestinal juice, were studied by dynamic dialysis system using TFu solution as control. The recovery rate of the method was determi-nated in different media. Results In case of solution, all the release profiles of TFu could be described by first order kinetics model and could be expressed by the following equations ： A = 37 602 C ＋ 160. 48（ r = 0. 999 9）, A = 39 488 C ＋ 1 915. 3（ r = 0. 999 8）,A = 38 790 C- 194. 11（ r = 0. 999 3）, respectively. In artificial gastric juice, the in vitro release behavior of chitosan modified TFu-SLNs could be expressed by the Ritger- Peppas equations： lnQ = 0. 398 4 lnt ＋ 3. 135 2（ r = 0. 979 6）. In artificial intestinal juice and artificial gastric juice followed by aritifical intestinal juice, the TFu release behavior of chitosan modified TFu- SLNs in vitro were both in accord with Weibull model： lnQ = 0. 385 2 ln t- 1. 325 86（ r = 0. 964 5） lnQ = 0. 412 6 lnt- 1. 270 2（ r = 0. 974 6）. Conclusion Chitosan Modified TFu- SLNs can release the drug slowly, and the drug release mechanism is dominated by drug diffusion.
出处
《中国药业》
CAS
2016年第9期12-14,共3页
China Pharmaceuticals
关键词
托氟啶
壳聚糖
体外释放度
N3-O-toluyl-flulorouracil（TFu）
chitosan
invitro release
