白藜芦醇-大麦醇溶蛋白复合纳米颗粒的光稳定性、 缓释行为及抗氧化能力

doi:10.7503/cjcu20150115

摘要/Abstract

摘要：

采用液-液分散法自组装制备了白藜芦醇-大麦醇溶蛋白复合纳米颗粒, 其平均粒径为(135.0±2.5) nm, 白藜芦醇包封率为90.4%, 负载率为18.8%; 扫描电子显微镜表征结果显示纳米颗粒表面光滑, 呈较规则的圆球状. 考察了复合纳米颗粒载体形式对白藜芦醇光稳定性的影响, 结果表明, 在紫外光下暴露18 h, 与游离白藜芦醇相比, 纳米颗粒中的白藜芦醇稳定性提高了26%. 通过模拟胃肠道环境考察了复合纳米颗粒的白藜芦醇缓释行为, 结果表明, 2 h内白藜芦醇在模拟胃液中的释放率为35%, 随后释放速率减慢, 6 h后的释放率为56%; 在模拟肠液中2 h内白藜芦醇的释放率为42%, 且在4 h内的释放行为遵循零级释放特征, 6 h后的释放率为88%. 对游离态白藜芦醇和复合纳米颗粒形式的白藜芦醇抗氧化能力进行了对比研究, 1,1-二苯基-2-苦肼基(DPPH)实验结果表明, 复合纳米颗粒形式的白藜芦醇比游离形式在清除氢过氧自由基方面能力稍强(IC₅₀值分别为0.4182 mmol/L和0.4378 mmol/L); HepG2细胞抗氧化模型实验进一步证实白藜芦醇在形成复合纳米颗粒后其抗氧化能力略有增强.

关键词: 白藜芦醇, 大麦醇溶蛋白, 纳米颗粒, 自组装

Abstract:

In order to protect the physiological activity of resveratrol, resveratrol-hordein nanoparticles were self-assembled by liquid-liquid dispersion method. The mean diameter of the nanoparticles[(135.0±2.5) nm] was measured with dynamic light scattering method, with encapsulation efficiency of resveratrol(90.4%) and drug loading(18.8%) were obtained by ultraviolet spectrophotometry method. Scanning electron microscope(SEM) showed that the morphology of nanoparticles was smooth and spherical. The effect of composite nanoparticles carrier type on the light stability of resvertrol was investigated. The results showed that the stability of resveratrol in nanoparticles was improved by 26% compared with that of free resveratrol after ultraviolet irradiation for 18 h. Resveratrol release behavior was studied in the simulated gastro-intestinal tract. The data revealed that 35% resveratrol was released from resveratrol-hordein nanoparticles in simulated gastric fluid at the first 2 h, and then released slowly, until 56% resveratrol was released after 6 h. While in the simulated intestinal fluid, 42% resveratrol was released in the first 2 h, and then steadily released from nanoparticles according to zero-order release kinetics during the first 4 h. After 6 h, 88% resveratrol was released. The antioxidant capability of free resvertrol and composite nanoparticles was studied. 1,1-Diphenyl-2-picrylhydrazyl radical(DPPH) experiment results showed that resvertrol in composite nanoparticles had a little more scavenging effect on DPPH free radicals(IC₅₀=0.4182 mmol/L) compared with free resvertrol(IC₅₀=0.4378 mmol/L). A HepG2 cellular antioxidant activity(CAA) assay further demonstrated the above results.

Key words: Resveratrol, Hordein, Nanoparticle, Self-assembly

中图分类号:

O625
TS201

TrendMD:

管骁, 殷婷, 韩飞. 白藜芦醇-大麦醇溶蛋白复合纳米颗粒的光稳定性、缓释行为及抗氧化能力. 高等学校化学学报, 2015, 36(9): 1707.

GUAN Xiao, YIN Ting, HAN Fei. Light Stability, Controlled-release and Antioxidation of Resveratrol-hordein Composite Nanoparticles^†. Chem. J. Chinese Universities, 2015, 36(9): 1707.

图/表 10

Fig.1 SEM image of resveratrol-hordein nanoparticles

Fig.2 FTIR spectra of resveratrol(a), hordein nanoparticles(b) and resveratrol-hordein nanoparticles(c)

Fig.3 Stability curve of resveratrol(a) and resveratrol-hordein nanoparticle(b) under UV-light exposure

Fig.4 Release profile of resveratrol in simulated gastric(a) and intestinal fluid(b)

Fig.5 Absorbance curves of DPPH under the conditions of coexistence with resveratrol(A) and resveratrol-hordein nanoparticles(B)

Fig.6 DPPH scavenging standard curves of resveratrol(a) and resveratrol-hordein nanoparticle(b)

Fig.7 Peroxyl radical-induced oxidation of DCFH to DCF in HepG2 cells and the inhibition of oxidation(A) Resveratrol; (B) resveratrol-hordein nanoparticles; (C) quercetin standard.c(Resveratrol)/(μmol·L-1): a. 0; b. 1; c. 5; d. 10; e. 20; f. 30; g. 40.

Fig.8 Dose-response curve for inhibition of peroxyl radical-induced DCFH oxidation(A) Resveratrol; (B) resveratrol-hordein nanoparticles; (C) quercetin standard.

Fig.9 Median effect plots for inhibition of peroxyl radical-induced DCFH oxidation(A) Resveratrol; (B) resveratrol-hordein nanoparticles; (C) quercetin standard.

Table 1 Comparison of cellular antioxidant activity between revertrol and revertrol-hordein nanoparticle

Antioxidant	EC₅₀/(μmol·L^-1)	CAA/[n(QE)/100 $n c *$ ]
Quercetin	6.41	100
Resveratrol	48.46	13.22
Resveratrol-hordein nanoparticles	45.31	14.14

Table 1 Comparison of cellular antioxidant activity between revertrol and revertrol-hordein nanoparticle

Antioxidant	EC₅₀/(μmol·L^-1)	CAA/[n(QE)/100 $n c *$ ]
Quercetin	6.41	100
Resveratrol	48.46	13.22
Resveratrol-hordein nanoparticles	45.31	14.14

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