基于紫胶-杏仁胶生物大分子的槲皮素载药纳米粒的自组装、功能及体外性质。
Self-assembly, functionality, and in-vitro properties of quercetin loaded nanoparticles based on shellac-almond gum biological macromolecules.
机构信息
Particle and Interfacial Technology Group (PaInT), Department of Green Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, Gent 9000, Belgium.
Particle and Interfacial Technology Group (PaInT), Department of Green Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, Gent 9000, Belgium.
出版信息
Int J Biol Macromol. 2019 May 15;129:1024-1033. doi: 10.1016/j.ijbiomac.2019.02.071. Epub 2019 Feb 19.
Quercetin-fortified nanoparticles were prepared from almond gum (AG), a novel biological macromolecule, and Tween 80 (T80) as stabilizers and shellac (SH) as core material using an antisolvent precipitation method. The final nanoparticles were prepared by 0.67% SH, 0.02% Q, 0.5% AG and 0.1% w/v T80 using the stirring speed of 750 rpm at a dosing rate of 0.5 ml/min. The morphology of the particles was characterized using Cryo-SEM and TEM microscopy. The average particle size was 135 ± 8 nm with a polydispersity index of 0.252 ± 0.01 and an encapsulation efficiency of 97.7 ± 1.2%. At pH 7.4 (intestinal pH), quercetin-loaded nanoparticles showed significantly (p < 0.05) higher antioxidant activity compared to free quercetin while the degradation of quercetin was lower in the nanoparticles compared to free quercetin at the similar pH. Quercetin loaded in nanoparticles was successfully found to be 2 times more available for uptake than free quercetin at pH 7.4. MTT and SRB assays revealed that no significant (p > 0.05) toxicity was observed for Caco-2 cells treated with quercetin-loaded nanoparticles with a dilution factor of 100. This study provides information about the formulation of promising nanocarriers using biological macromolecules for oral delivery of bioactive compounds.
杏仁胶（AG）是一种新型生物大分子，用它和 Twee80（T80）作为稳定剂，紫胶（SH）作为芯材，通过抗溶剂沉淀法制备了富含槲皮素的纳米颗粒。最终的纳米颗粒由 0.67%的 SH、0.02%的 Q、0.5%的 AG 和 0.1%的 w/v T80 组成，搅拌速度为 750 rpm，剂量率为 0.5 ml/min。使用 Cryo-SEM 和 TEM 显微镜对颗粒的形态进行了表征。颗粒的平均粒径为 135 ± 8nm，多分散指数为 0.252 ± 0.01，包封效率为 97.7 ± 1.2%。在 pH 7.4（肠内 pH）时，与游离槲皮素相比，载有槲皮素的纳米颗粒显示出显著（p < 0.05）更高的抗氧化活性，而在类似 pH 下，纳米颗粒中的槲皮素降解率低于游离槲皮素。与游离槲皮素相比，在 pH 7.4 时，载于纳米颗粒中的槲皮素被证明更易被细胞摄取，可达 2 倍。MTT 和 SRB 检测结果表明，用稀释因子为 100 的载有槲皮素的纳米颗粒处理 Caco-2 细胞时，没有观察到显著的（p > 0.05）毒性。该研究提供了关于使用生物大分子为生物活性化合物的口服给药来制备有前途的纳米载体的信息。
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