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纳米耳蜗作为一种新型给药载体,可提高二氢杨梅素在胃肠道中的水溶性、稳定性和控制释放。

Nanocochleates as novel delivery vehicles for enhancement of water solubility, stability and controlled release of dihydromyricetin in gastrointestinal tract.

机构信息

School of Agricultural Engineering and Food Science, Shandong University of Technology, Xincun West Road, Zibo, Shandong Province 255000, PR China.

School of Agricultural Engineering and Food Science, Shandong University of Technology, Xincun West Road, Zibo, Shandong Province 255000, PR China.

出版信息

Food Res Int. 2024 Dec;197(Pt 1):115174. doi: 10.1016/j.foodres.2024.115174. Epub 2024 Sep 29.

DOI:10.1016/j.foodres.2024.115174
PMID:39593385
Abstract

Dihydromyricetin (DHM) possesses impressive antioxidant and anti-inflammatory properties; however, its effectiveness is limited by poor bioavailability. Liposomes improve the solubility and stability of insoluble bioactives but encounter challenges in gastrointestinal fluids after oral administration. Consequently, DHM-loaded nanocochleates were fabricated to enhance the solubility, stability, and release behavior of DHM. The nanoliposomes exhibited an entrapment efficiency (EE) ranging from 85.64 % to 88.79 %, a particle size between 136.20 and 150.70 nm, a polydispersity index (PDI) of 0.36 to 0.43, and a zeta potential of -6.82 to -11.13 mV. In contrast, the cylindrical-shaped nanocochleates demonstrated an EE ranging from 74.94 % to 84.64 %, a particle size between 239.07 and 571.43 nm, a PDI from 0.16 to 0.61, and a zeta potential ranging from -21.97 to -27.10 mV. The nanocochleates exhibited improved water solubility (64.75 %) and retained antioxidant activity (41.38 %) compared to free DHM. Additionally, they demonstrated enhanced stability of DHM compared to nanoliposomes during 30 days of storage. Fourier transform infrared spectroscopy and differential scanning calorimetry confirmed that DHM was encapsulated within nanocochleate structures via ionic and chemical interactions. X-ray diffraction revealed a distinct organization of the nanocochleates in comparison to the nanoliposomes. The release of DHM from nanocochleates demonstrated a prolonged and controlled release in simulated gastrointestinal medium, unlike the burst release observed with nanoliposomes. This study hightlighted the potential of nanocochleates as novel delivery vehicles for enhancing the stability and bioavailability of DHM. It also offered a unique perspective on developing functional food formulations that utilize nanocochleates as promising nanocarriers for bioactives.

摘要

二氢杨梅素(DHM)具有显著的抗氧化和抗炎特性;然而,其功效受到生物利用度差的限制。脂质体可以提高难溶性生物活性物质的溶解度和稳定性,但在口服后遇到胃肠道液体时会遇到挑战。因此,制备了载 DHM 的纳米笼形物以提高 DHM 的溶解度、稳定性和释放行为。纳米脂质体的包封效率(EE)在 85.64%至 88.79%之间,粒径在 136.20 至 150.70nm 之间,多分散指数(PDI)在 0.36 至 0.43 之间,zeta 电位在-6.82 至-11.13mV 之间。相比之下,圆柱形纳米笼形物的 EE 范围为 74.94%至 84.64%,粒径在 239.07nm 至 571.43nm 之间,PDI 在 0.16 至 0.61 之间,zeta 电位在-21.97 至-27.10mV 之间。与游离 DHM 相比,纳米笼形物具有更高的水溶性(64.75%)和保留的抗氧化活性(41.38%)。此外,与纳米脂质体相比,它们在 30 天的储存过程中表现出更好的 DHM 稳定性。傅里叶变换红外光谱和差示扫描量热法证实,DHM 通过离子和化学相互作用被包封在纳米笼形物结构中。X 射线衍射表明,与纳米脂质体相比,纳米笼形物具有明显的组织。与纳米脂质体的爆发式释放不同,DHM 从纳米笼形物中的释放呈现出延长和控制的释放。这项研究强调了纳米笼形物作为新型递送载体的潜力,可提高 DHM 的稳定性和生物利用度。它还为开发功能性食品配方提供了一个独特的视角,利用纳米笼形物作为有前途的生物活性物质的纳米载体。

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