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姜黄素负载于棕榈硬脂酸和胆固醇固体脂质纳米粒微胶囊中,提高了其体内稳定性和生物利用度。

Fucoxanthin Loaded in Palm Stearin- and Cholesterol-Based Solid Lipid Nanoparticle-Microcapsules, with Improved Stability and Bioavailability In Vivo.

机构信息

College of Food Science, Fujian Agriculture and Forestry University, Fuzhou 350002, China.

Technical Innovation Center for Utilization of Marine Biological Resources, Third Institute of Oceanography, Ministry of Natural Resources, Xiamen 361005, China.

出版信息

Mar Drugs. 2022 Mar 29;20(4):237. doi: 10.3390/md20040237.

Abstract

Fucoxanthin (FX) is a marine carotenoid that has proven to be a promising marine drug due to the multiple bioactivities it possesses. However, the instability and poor bioavailability of FX greatly limit its application in pharmaceuticals or functional foods. In this study, the creative construction of a solid lipid nanoparticle-microcapsule delivery system using mixed lipids of palm stearin and cholesterol wrapped with gelatin/Arabic gum to load lipophilic FX was fabricated, aiming to improve the stability and bioavailability of FX. The results showed that the encapsulated efficiency (EE) and drug loading capacity (LC) of optimized FX microcapsules (FX-MCs) obtained were as high as 96.24 ± 4.60% and 0.85 ± 0.04%, respectively, after single-factor experiments. The average particle size was 1154 ± 54 nm with negative Zeta potential (-20.71 ± 0.93 mV) as depicted with size-zeta potential spectrometer. The differential scanning calorimeter (DSC) and thermogravimetric analyzer (TG) results indicated that FX-MC has a higher Tg and slower weight loss than FX monomers (FX crystal) and blank MCs. Besides, The Fourier transform infrared spectrometer (FTIR) confirmed the good double encapsulation of FX into the solid lipid and composite coacervate. Moreover, the encapsulated FX showed higher storage stability, sustained release (55.02 ± 2.80% release in 8 h), and significantly improved bioavailability (712.33%) when compared to free FX. The research results can provide a principle theoretical basis for the development and application of FX in pharmaceuticals or functional foods.

摘要

岩藻黄质(FX)是一种海洋类胡萝卜素,由于其具有多种生物活性,已被证明是一种很有前途的海洋药物。然而,FX 的不稳定性和生物利用度差极大地限制了它在药物或功能性食品中的应用。在本研究中,创造性地构建了一种使用混合棕榈硬脂和胆固醇的固体脂质纳米粒-微胶囊递送系统,用明胶/阿拉伯胶包裹,以负载亲脂性 FX,旨在提高 FX 的稳定性和生物利用度。结果表明,通过单因素实验,优化后的 FX 微胶囊(FX-MC)的包封效率(EE)和载药量(LC)分别高达 96.24±4.60%和 0.85±0.04%。平均粒径为 1154±54nm,带有负 ζ 电位(-20.71±0.93mV),如粒径-ζ 电位光谱仪所示。差示扫描量热仪(DSC)和热重分析仪(TG)结果表明,与 FX 单体(FX 晶体)和空白 MC 相比,FX-MC 的 Tg 更高,重量损失更慢。此外,傅里叶变换红外光谱(FTIR)证实了 FX 被良好地双重包封在固体脂质和复合凝聚物中。此外,与游离 FX 相比,包封的 FX 表现出更高的储存稳定性、持续释放(8 小时内释放 55.02±2.80%)和显著提高的生物利用度(712.33%)。研究结果可为 FX 在药物或功能性食品中的开发和应用提供原理性的理论基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ec3a/9032552/de630972a576/marinedrugs-20-00237-g001.jpg

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