载槲皮素-粉防己碱纳米凝胶的制备、表征与体外评价

Preparation and characterization of quercetin-tetrandrine nanoparticle and evaluation in vitro and in vivo

关键词:  槲皮素  粉防己碱  纳米凝胶  抗氧化  超声雾化

Key words:  quercetin  tetrandrine  nanoparticle  anti-oxidant  ultrasonic atomization

摘要:

[目的] 制备一种纳米凝胶制剂以提高槲皮素及粉防己碱的生物利用度及抗氧化性。[方法] 通过反相乳化法制备载槲皮素-粉防己碱纳米凝胶（QU-TE-NP）；通过粒径与Zeta电位测定，透射电子显微镜（TEM），差示扫描量热分析（DSC）以及傅里叶变换红外光谱（FT-IR）进行表征分析；高效液相法测定两种药物的载药率及包封率；1，1-二苯基-2-三硝基苯肼（DPPH）清除实验比较槲皮素及该纳米凝胶的体外抗氧化性。[结果] 该纳米凝胶通过钙离子交联，平均粒径为（38.86±1.81） nm，Zeta电位为（-15.9±4.1） mV，槲皮素和粉防己碱的载药率分别为（0.98±0.04）%和（2.75±0.07）%，包封率分别为（96.80±1.10）%和（94.80±0.90）%。纳米凝胶的抗氧化性明显优于槲皮素单体。[结论] 纳米凝胶体系的制备可提高槲皮素及粉防己碱的水溶性，并增强其抗氧化能力。

Abstract:

[Objective] To prepare a nanoparticle to improve the bioavailability and antioxidant activity of quercetin and tetrandrine.[Methods] The quercetin-tetrandrine-nanoparticle (QU-TE-NP) was prepared by reverse microemulsion method. The QU-TE-NP was characterized by particle size and zeta potential analysis, transmission electron microscope (TEM), differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FT-IR). The drug loading and encapsulation efficiency were measured by high performance liquid chromatography (HPLC). The antioxidant activities of quercetin and QU-TE-NP were compared by DPPH radical scavenging experiment.[Results] The nanoparticles formed a stable new phase by cross-linking. The average particle size was (38.86 ±1.81) nm and the Zeta potential was (-15.9±4.1) mV. The drug loading and entrapment efficiency of quercetin and tetrandrine were (0.98±0.04)%, (2.75±0.07)%, (96.80±1.10)%, (94.80±0.90)%, respectively. The antioxidant activity of QU-TE-NP was superior to quercetin.[Conclusion] The QU-TE-NP formulation enhanced the water-solubility of quercetin and tetrandrine, resulting in improved antioxidant capacity.