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丝蛋白衍生的 N-月桂酰基氨基酸可以与阿糖胞苷形成双离子复合物,作为新型抗肿瘤药物传递系统。

Sodium N-lauryl amino acids derived from silk protein can form catanionic aggregates with cytarabine as novel anti-tumor drug delivery systems.

机构信息

Silk Biotechnology Laboratory, School of Biology and Basic Medical Sciences, Soochow University, Suzhou, China.

National Engineering Laboratory for Modern Silk, Soochow University, Suzhou, China.

出版信息

Drug Deliv. 2020 Dec;27(1):482-490. doi: 10.1080/10717544.2020.1742250.

Abstract

A sodium N-lauryl amino acids (shortly silk sericin surfactant, SSS) is synthesized with lauryl chloride and sericin amino acids recovered from silk industrial waste. The purpose of this study is to explore whether the sericin surfactant can be used as a potential drug delivery carrier. By controlling the proportion of cationic drugs, cytarabine hydrochloride (CH) and anionic SSS, the aggregation behavior, slow release capability and toxicological effects of catanionic aggregates or vesicles, formed through CH and SSS, have been investigated in detail. Dynamic light scattering (DLS), transmission electron microscopy (TEM), and zeta potential analysis showed that the aggregate solution could form a stable vesicle structure when the mass fraction of CH is less than or equal to 0.3. The drug release results showed that the cumulative release rate of the catanionic aggregation solution with CH mass fraction of 0.2 reached a maximum at 18 h, being approximately 9 times greater than that of pure cytarabine. The CH/SSS aggregates had a significant sustained release effect compared with the control group. At the same time, vesicles formed by SSS and CH have better anti-tumor effects compared with the pure drug group. In summary, sericin surfactant from silk industrial waste has a potential use as a drug delivery carrier.

摘要

一种 N-月桂酰基氨基酸钠(简称丝胶氨基酸表面活性剂,SSS)是由月桂酰氯和从丝工业废料中回收的丝胶氨基酸合成的。本研究旨在探讨丝胶表面活性剂是否可用作潜在的药物传递载体。通过控制阳离子药物盐酸阿糖胞苷(CH)和阴离子 SSS 的比例,详细研究了 CH 和 SSS 形成的 CATANIONIC 聚集物或囊泡的聚集行为、缓慢释放能力和毒理学效应。动态光散射(DLS)、透射电子显微镜(TEM)和zeta 电位分析表明,当 CH 的质量分数小于或等于 0.3 时,聚集溶液可以形成稳定的囊泡结构。药物释放结果表明,CH 质量分数为 0.2 的 CATANIONIC 聚集溶液的累积释放率在 18 小时达到最大值,约为纯阿糖胞苷的 9 倍。与对照组相比,CH/SSS 聚集物具有明显的持续释放效果。同时,由 SSS 和 CH 形成的囊泡比纯药物组具有更好的抗肿瘤效果。综上所述,丝工业废料中的丝胶表面活性剂具有作为药物传递载体的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/974f/7170395/7a02a6cdf153/IDRD_A_1742250_F0001_C.jpg

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