柑橘生物质生物类黄酮缓释双层体系的制备与表征

IF 4.6 Q1 CHEMISTRY, APPLIED
Niharika Kaushal, Minni Singh
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引用次数: 1

摘要

食品级水凝胶是由公认安全(GRAS)聚合物制备的,是很有前途的递送系统。本研究研究了海藻酸盐水凝胶对含黄酮类化合物的聚乳酸-羟基乙酸(PLGA)纳米颗粒的支持能力,并通过体外胃肠道环境观察了其随后的释放模式。从柑桔皮中提取黄酮类化合物,主要由多甲氧基黄酮类化合物和黄酮类化合物组成,主要由橘皮素和枳实素组成。将其纳入由GRAS分类的PLGA制备的纳米颗粒(以下简称类黄酮-PLGA纳米颗粒)中,提供第一层保护,然后将其嵌入海藻酸盐水凝胶中,提供第二层保护。这种双层系统的开发是为了确保生物活性物质通过恶劣的胃环境的安全通道,否则会导致黄酮类化合物的全身前代谢,使其无效。对凝胶进行了表征,6.0%海藻酸盐水凝胶被认为是最佳的,因为它提供了密集的网络,正如场发射扫描电镜(FE-SEM)图像所证实的那样,而且孔隙率低,确保了纳米颗粒的保留。凝胶流变学揭示了水凝胶的剪切变薄行为,在500N载荷下,6%的水凝胶具有较高的抗变形能力。经质谱分析(MS)证实,在胃肠道环境中,在胃相的前2小时,类黄酮的释放可忽略不计,为4.0%,随后在肠道环境中持续释放10小时。水凝胶的共聚焦激光扫描显微镜(CLSM)图像清楚地显示了ph响应性肿胀和纳米颗粒在肠期从水凝胶释放。据设想,这些和其他类似的发现最终将体现在“功能性水凝胶”输送系统中,该系统能够在保留其功能的同时纳入营养保健品,并在不久的将来作为可行的产品。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Fabrication and characterization of a bilayered system enabling sustained release of bioflavonoids derived from mandarin biomass

Fabrication and characterization of a bilayered system enabling sustained release of bioflavonoids derived from mandarin biomass

Food-grade hydrogels, those prepared with Generally Recognized as Safe (GRAS) polymers, are promising delivery systems. In this work, alginate hydrogels were studied for their ability to uphold flavonoids laden poly-lactic-co-glycolic acid (PLGA) nanoparticles, and their subsequent release pattern was observed through in vitro gastrointestinal environments. Flavonoids were derived from mandarin peels, and consisted of polymethoxyflavones, chiefly tangeretin and nobiletin, and flavanones, chiefly naringenin. Incorporating these into nanoparticles prepared from GRAS classified PLGA, hereinafter referred to as flavonoids-PLGA nanoparticles, offered the first layer of protection, which were then embedded into alginate hydrogels, offering the second layer of protection. This bilayered system was developed to ensure guarded passage of the bioactives through the severe gastric environment, which would otherwise lead to presystemic metabolism of the flavonoids, rendering them ineffective. The gels were characterised and a 6.0% alginate hydrogel was considered optimal as it offered a dense network, as confirmed by a field emission scanning electron microscope (FE-SEM) image, and a low porosity, which ensured retention of the nanoparticles. Gel rheology revealed the shear thinning behavior of hydrogels, and high resistance to deformation was observed for 6% hydrogel when subjected to a load of 500N. Subjecting the ensemble to gastrointestinal environments showed a negligible 4.0% release of flavonoids in the first 2 hours of the gastric phase, followed by a sustained release through the next 10 hours in the intestinal environment, as confirmed by mass spectrometry (MS) profiles. Confocal laser scanning microscope (CLSM) images of the hydrogel clearly revealed the pH-responsive swelling and release of the nanoparticles from the hydrogel in the intestinal phase. It is envisaged that these, and other similar findings, would eventually manifest into ‘functional hydrogels’ delivery systems that bear the ability to incorporate nutraceuticals whilst retaining their functionality, as viable products in the near future.

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