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乙酰化麦芽糊精纳米粒的制剂特性、酸可调降解性和细胞相互作用。

Formulation attributes, acid tunable degradability and cellular interaction of acetalated maltodextrin nanoparticles.

机构信息

Department of Pharmacy, Biopharmaceutics and Pharmaceutical Technology, Saarland University, 66123 Saarbrücken, Germany.

Department of Pharmacy, Pharmaceutical Biology, Saarland University, 66123 Saarbrücken, Germany.

出版信息

Carbohydr Polym. 2022 Jul 15;288:119378. doi: 10.1016/j.carbpol.2022.119378. Epub 2022 Mar 22.

Abstract

Exploiting materials for nanoparticle production has never halted to address the diversity in cargos and applications. Herein, maltodextrin (MD) was selected for being economic, nontoxic, biocompatible, and biodegradable. Different MDs were modified through acetal modification, turning the polymer hydrophobic and allowing pH-dependent tunable degradability. The synthesized acetalated MD (AcMD) polymers exhibited different thermal decomposition profiles and lower glass transition temperatures. Nanoprecipitation yielded uniform AcMD nanoparticles (NPs) with diameters ranging from 141 to 258 nm. The particles were loaded with hydrophobic model drug, resveratrol (67.86% entrapment efficiency and 3.75% drug loading). The degradation and the in vitro release were studied at pH 7.4 and pH 5.0 and revealed different kinetics in dependence on the amount of cyclic/acyclic acetalation. Cell viability and cellular interaction were studied on adenocarcinoma human lung epithelial A549 and differentiated human monocytic THP-1 cells. The AcMD-NPs were well tolerated by both cell lines but exhibited different uptake behaviors.

摘要

为了满足不同货物和应用的多样性需求,用于纳米颗粒生产的材料的开发从未停止过。在此,选择麦芽糊精(MD)是因为它经济、无毒、生物相容和可生物降解。通过缩醛改性对不同的 MD 进行改性,使聚合物具有疏水性,并允许 pH 依赖性的可调降解性。合成的乙酰化 MD(AcMD)聚合物表现出不同的热分解曲线和更低的玻璃化转变温度。纳米沉淀得到直径在 141 到 258nm 之间的均匀 AcMD 纳米颗粒(NPs)。这些颗粒负载疏水性模型药物白藜芦醇(包封效率为 67.86%,载药量为 3.75%)。在 pH7.4 和 pH5.0 下研究了降解和体外释放,发现其动力学取决于环状/非环状缩醛化的数量。在人肺腺癌细胞 A549 和分化的人单核细胞 THP-1 细胞上研究了细胞活力和细胞相互作用。AcMD-NPs 被这两种细胞系均耐受,但表现出不同的摄取行为。

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