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壳聚糖修饰介孔硅纳米载药系统的制备、表征及体外释放性能

Delivery of curcumin by fucoidan-coated mesoporous silica nanoparticles: Fabrication, characterization, and in vitro release performance.

机构信息

School of Food and Pharmacy, Zhejiang Ocean University, Zhoushan 316022, PR China.

School of Food and Pharmacy, Zhejiang Ocean University, Zhoushan 316022, PR China.

出版信息

Int J Biol Macromol. 2022 Jun 30;211:368-379. doi: 10.1016/j.ijbiomac.2022.05.086. Epub 2022 May 14.

Abstract

Mesoporous silica nanoparticles (MSN) are effective drug delivery carriers because of their adjustable large pore size and high porosity. In this study, complex nanoparticles containing disulfide bonds (SS) were designed and prepared as curcumin (Cur) carriers by using fucoidan (FUC) and MSN as the polymer matrix. The product was characterized using scanning electron microscopy, transmission electron microscopy, dynamic light scattering, Fourier-transform infrared spectroscopy, and an N adsorption and desorption test. When the mass ratio of MSN to FUC was 2:1, the nanospheres particle size was the smallest (295.6 ± 0.98 nm, -35.2 ± 0.8 mV). Furthermore, the curcumin encapsulation rate by MSN-Cur-SS-FUC was over 90%, and the cumulative release rate in 24 h was over 80% due to the combined effect of weak acidity and high glutathione concentration in the tumor site microenvironment. When the Cur concentration was 50 μg/mL, the cell viability of free Cur was 63.8%, the cell viability of MSN-Cur-SS-FUC was 14.5%, and the cell viability of MSN-SS-FUC at the same concentration remained above 74.6%. MSN-SS-FUC composite nanoparticles showed a good delivery of Cur, a lipid-soluble active compound, and provides a new delivery route for other lipid-soluble and poorly bioavailable active compounds.

摘要

介孔硅纳米粒子(MSN)由于其可调的大孔径和高孔隙率,是有效的药物传递载体。在这项研究中,设计并制备了含有二硫键(SS)的复合纳米粒子作为姜黄素(Cur)载体,使用褐藻糖胶(FUC)和 MSN 作为聚合物基质。使用扫描电子显微镜、透射电子显微镜、动态光散射、傅里叶变换红外光谱和 N 吸附和解吸测试对产物进行了表征。当 MSN 与 FUC 的质量比为 2:1 时,纳米球的粒径最小(295.6±0.98nm,-35.2±0.8mV)。此外,由于肿瘤部位微环境中弱酸性和高谷胱甘肽浓度的综合作用,MSN-Cur-SS-FUC 的姜黄素包封率超过 90%,24 小时内的累积释放率超过 80%。当 Cur 浓度为 50μg/mL 时,游离 Cur 的细胞活力为 63.8%,MSN-Cur-SS-FUC 的细胞活力为 14.5%,相同浓度下 MSN-SS-FUC 的细胞活力保持在 74.6%以上。MSN-SS-FUC 复合纳米粒子对脂溶性活性化合物 Cur 具有良好的传递作用,为其他脂溶性和生物利用度差的活性化合物提供了新的传递途径。

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