负载紫檀芪的岩藻多糖-小麦醇溶蛋白纳米颗粒的制备及体外抗肝癌活性研究

Preparation and Anti-hepatoma Activity in vitro of Pterostilbene Loaded with Fucoidan-Gliadin Nanoparticles

紫檀芪是一种具有多种生物活性的疏水性天然产物,因低溶解度和光不稳定性而限制了其在实际中的应用。通过pH驱动法制备了具岩藻多糖涂层的小麦醇溶蛋白纳米颗粒,确定了小麦醇溶蛋白与岩藻多糖的最优质量比为8∶1,以该纳米颗粒为载体包封了紫檀芪,确定了紫檀芪与小麦醇溶蛋白的最优质量比为1∶10,最终制得的紫檀芪-小麦醇溶蛋白-岩藻多糖纳米颗粒呈近似球形,粒径为(122.34±1.08)nm,PDI为0.188±0.001,Zeta电位为(-27.73±0.44)mV,包封率为(94.09±1.60)%,载药率为(8.36±0.14)%,在pH为3.0~8.0的溶液和NaCl浓度为0~20 mmol/L的溶液中具良好的稳定性,长期储存稳定性良好,光照稳定性显著强于游离的紫檀芪;红外实验表明小麦醇溶蛋白、紫檀芪、岩藻多糖三者之间主要通过静电吸引、氢键和疏水作用结合。HepG2细胞的MTT实验和凋亡实验表明,与游离紫檀芪相比,紫檀芪-小麦醇溶蛋白-岩藻多糖纳米颗粒具有显著提高的体外抗肝癌活性。

Pterostilbene was a hydrophobic natural product with various biological activities.However,the low solubility and light instability of pterostilbene limit its application in practice.Gliadin nanoparticles coated with fucoidan was prepared by pH driving method,and it was determined that the optimal mass ratio of gliadin to fucoidan was 8∶1.The above-mentioned nanoparticles were used as the carrier to encapsulate pterostilbene,and it was determined that the optimal mass ratio of pterostilbene to gliadin was 1∶10.The final pterostilbene-gliadin-fucoidan nanoparticles was approximately spherical in shape,with particle size of(122.34±1.08)nm,PDI of 0.188±0.001,Zeta potential of(-27.77±0.44)mV,encapsulation rate of(94.09±1.60)%,and drug loading rate of(8.36±0.14)%.It had a good stability in pH 3.0~8.0 solution and solution with NaCl concentration of 0~20 mmol/L,a good long-term storage stability,and its light stability was stronger than that of free pterostilbene significantly.Infrared experiment showed that gliadin,pterostilbene and fucoidan were mainly combined by electrostatic attraction,hydrogen bond and hydrophobic interaction.MTT test and apoptosis test of HepG2 cells revealed that the anti-hepatoma activity of pterostilbene-gliadin-fucoidan nanoparticles was better than that of free pterostilbene in vitro dramatically.