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负载牡荆素的聚乙二醇甲醚接枝壳聚糖/海藻酸钠纳米粒:制备、理化性质及体外释放行为

Vitexin-loaded poly(ethylene glycol) methyl ether-grafted chitosan/alginate nanoparticles: preparation, physicochemical properties and in vitro release behaviors.

作者信息

Yoksan Rangrong, Towongphaichayonte Pawika

机构信息

Department of Packaging and Materials Technology, Faculty of Agro-Industry, Kasetsart University, Bangkok, Thailand.

Center for Advanced Studies for Agriculture and Food, Kasetsart University Institute for Advanced Studies, Kasetsart University, Bangkok, Thailand.

出版信息

J Sci Food Agric. 2024 Jan 30;104(2):956-966. doi: 10.1002/jsfa.12984. Epub 2023 Sep 29.

Abstract

BACKGROUND

Vitexin, a flavonoid in various foods and medicinal plants, has potential clinical, therapeutic and food applications due to its bioactive properties and beneficial health effects. However, its poor water solubility causes low oral bioavailability and poor absorption in the gastrointestinal tract, limiting its practical applications. Encapsulation is an efficient approach to overcome these limitations. This study demonstrates the encapsulation of vitexin into poly(ethylene glycol) methyl ether-grafted chitosan (mPEG-g-CTS)/alginate (ALG) polyelectrolyte complex nanoparticles.

RESULTS

The vitexin-loaded mPEG-g-CTS/ALG nanoparticles were characterized by Fourier transform infrared spectroscopy, ultraviolet-visible spectroscopy and X-ray diffraction. The vitexin-loaded mPEG-g-CTS/ALG nanoparticles had a spherical shape, 50-200 nm in diameter, and negatively charged surface (-27 to -38 mV). They possessed a loading capacity of 4-60%, encapsulation efficiency of 50-100% and antioxidant activity (30-52% 2,2-diphenyl-1-picrylhydrazyl decoloration) when their initial vitexin content was 0.02-0.64 g g polymers. Successful vitexin loading into mPEG-g-CTS/ALG nanoparticles was also indirectly confirmed by the enhanced thermal stability of both polymers and the residual soybean oil used in the emulsion preparation step and delayed oxidative degradation of the residual soybean oil. Vitexin's in vitro release from the mPEG-g-CTS/ALG nanoparticles was very fast in phosphate buffer at pH 11, followed by pH 7, and very slow in acetate buffer at pH 3. The gastrointestinal digestion of vitexin increased by encapsulating into mPEG-g-CTS/ALG nanoparticles.

CONCLUSIONS

Vitexin-loaded mPEG-g-CTS/ALG nanoparticles were successfully fabricated using a two-step process of oil-in-water emulsion and ionic gelation without the use of pungent odor acids and other crosslinkers. The obtained nanoparticles are suitable for oral intestinal-specific delivery systems. © 2023 Society of Chemical Industry.

摘要

背景

牡荆素是多种食物和药用植物中的一种黄酮类化合物,因其生物活性特性和有益健康的作用而具有潜在的临床、治疗和食品应用价值。然而,其水溶性差导致口服生物利用度低且在胃肠道中吸收不良,限制了其实际应用。包封是克服这些限制的有效方法。本研究展示了将牡荆素包封到聚(乙二醇)甲醚接枝壳聚糖(mPEG-g-CTS)/海藻酸盐(ALG)聚电解质复合纳米颗粒中的过程。

结果

通过傅里叶变换红外光谱、紫外可见光谱和X射线衍射对负载牡荆素的mPEG-g-CTS/ALG纳米颗粒进行了表征。负载牡荆素的mPEG-g-CTS/ALG纳米颗粒呈球形,直径为50 - 200nm,表面带负电荷(-27至-38mV)。当初始牡荆素含量为0.02 - 0.64g/g聚合物时,它们的载药量为4 - 60%,包封率为50 - 100%,且具有抗氧化活性(2,2-二苯基-1-苦基肼脱色率为30 - 52%)。聚合物以及乳液制备步骤中使用的残留大豆油热稳定性的提高以及残留大豆油氧化降解的延迟也间接证实了牡荆素成功负载到mPEG-g-CTS/ALG纳米颗粒中。牡荆素从mPEG-g-CTS/ALG纳米颗粒中的体外释放在pH 11的磷酸盐缓冲液中非常快,其次是pH 7,而在pH 3的醋酸盐缓冲液中非常缓慢。通过包封到mPEG-g-CTS/ALG纳米颗粒中,牡荆素的胃肠道消化率提高。

结论

采用水包油乳液和离子凝胶两步法,无需使用刺鼻气味的酸和其他交联剂,成功制备了负载牡荆素的mPEG-g-CTS/ALG纳米颗粒。所得纳米颗粒适用于口服肠道特异性递送系统。© 2023化学工业协会。

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