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肽组装水凝胶用于 pH 可控药物释放。

Peptide-assembled hydrogels for pH-controllable drug release.

机构信息

School of Chemistry and Materials Science, Ludong University, Yantai, 264025, China.

Key Laboratory of Colloid and Interface Chemistry & Key Laboratory of Special Aggregated Materials, Shandong University, Ministry of Education, Jinan, 250100, China.

出版信息

Colloids Surf B Biointerfaces. 2020 Jan 1;185:110567. doi: 10.1016/j.colsurfb.2019.110567. Epub 2019 Oct 12.

Abstract

A peptide (FFACD) can form hydrogels in DMSO-HO mixtures (G1), NaOH (G2) and L-arginine (G3) aqueous solutions, respectively. Methyl thiazolyl tetrazolium (MTT) assays demonstrated that G1 and G3 exhibited excellent biocompatibility against HEK293 epithelial cells while G2 had an obvious cytotoxicity. G1 and G3 were used as drug carriers with the high drug loading capacity (DLC). Both hydrophilic DOX and hydrophobic PTX were completely loaded into G1 without destroying the hydrogel, while G3 could only encapsulate DOX. The strong electrostatic interaction between DOX and FFACD molecules could destroy the microstructure of G3 to produce precipitate with a high DOX DLC of 93%. The cytotoxicity assay of G1/DOX against K562 leukemia cells indicated that G1 did not inhabit the efficacy of DOX. In vitro release experiments demonstrated DOX of G3/DOX precipitates could be released 76% at pH = 6.0 of the tumor cells and only about 13% at pH = 7.4 of normal cells.

摘要

一种肽(FFACD)可以分别在 DMSO-HO 混合物(G1)、NaOH(G2)和 L-精氨酸(G3)水溶液中形成水凝胶。噻唑蓝(MTT)测定表明,G1 和 G3 对 HEK293 上皮细胞表现出优异的生物相容性,而 G2 具有明显的细胞毒性。G1 和 G3 被用作具有高载药能力(DLC)的药物载体。亲水性 DOX 和疏水性 PTX 都可以完全加载到 G1 中而不会破坏水凝胶,而 G3 只能包封 DOX。DOX 和 FFACD 分子之间的强静电相互作用可以破坏 G3 的微观结构,产生具有 93%高 DOX DLC 的沉淀。G1/DOX 对 K562 白血病细胞的细胞毒性试验表明,G1 不抑制 DOX 的功效。体外释放实验表明,G3/DOX 沉淀中的 DOX 在 pH = 6.0 的肿瘤细胞中可以释放 76%,而在 pH = 7.4 的正常细胞中仅释放约 13%。

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