反式白藜芦醇纳米粒的制备及其体外评价

Preparation and In Vitro Evaluation of Trans-Resveratrol Nanoparticles

采用离子交联法制备反式白藜芦醇纳米粒(t-Res-NPs),通过Box-Behnken效应面法优化制备工艺.从包封率、粒径、Zeta电位、载药量、纳米粒形态、缓释作用、稳定性等方面对t-Res-NPs进行体外评价.结果表明:t-Res-NPs粒径为(85.38±1.69) nm,Zeta电位为(19.93±3.25) mV,包封率为(88.31±0.59)%,载药量为(5.96±1.60)%;纳米粒形态呈圆形;t-Res-NPs具有良好的缓释作用,释放过程较为平稳,突释现象不明显;肠内菌对t-Res-NPs及反式白藜芦醇(t-Res)几乎无代谢作用,肝脏代谢酶对t-Res具有强烈的代谢作用,而t-Res-NPs可以有效地保护药物,减慢其代谢速率;t-Res-NPs可明显改善t-Res溶解度差、生物利用度低的缺点.

Trans-resveratrol nanoparticles(t-Res-NPs) were prepared by ion-crosslinking, and the preparation process was optimized by Box-Behnken effect surface method. t-Res-NPs were evaluated in vitro from the aspects of encapsulation efficiency, particle size, Zeta potential, drug loading, nanoparticle morphology, sustained release and stability. The results show that the prepared t-Res-NPs have particle size of(85.38±1.69) nm, Zeta potential of(19.93±3.25) mV, entrapment efficiency of(88.31±0.59)%, and the drug loading of(5.96±1.60)%;the nanoparticle morphology is round;t-Res-NPs have a good sustained release effect, and the release process is relatively stable, which has no obvious burst release phenomenon;intestinal bacteria have almost no metabolism to t-Res-NPs and trans-resveratrol(t-Res), while liver metabolic enzymes have a strong metabolic effect on t-Res, and t-Res-NPs can protect the drug effectively and slow down its metabolic rate;t-Res-NPs can improve the poor solubility and low bioavailability of t-Res significantly.