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胆碱支持的聚离子液体接枝共聚物作为阴离子药物的新型递药系统用于抗炎和抗凝血治疗。

Choline supported poly(ionic liquid) graft copolymers as novel delivery systems of anionic pharmaceuticals for anti-inflammatory and anti-coagulant therapy.

机构信息

Department of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, Strzody 9, 44-100, Gliwice, Poland.

Biosystems Group, Institute of Automatic Control, Faculty of Automatics, Electronics, and Informatics, Silesian University of Technology, Akademicka 16, Gliwice, Poland.

出版信息

Sci Rep. 2019 Oct 8;9(1):14410. doi: 10.1038/s41598-019-50896-5.

Abstract

New type of carriers based on grafted poly(ionic liquid)s was designed for delivery of ionically attached salicylates (Sal). Choline derived ionic liquid monomeric units were successfully introduced with various content in the side chains by the controlled radical polymerization. Properly high amounts of ionic pharmaceutics in the polymer systems were achieved by the well-fitted length and grafting degree of the side chains. In aqueous solution the graft copolymers were self-assembled into the spherical superstructures with sizes up to 73 nm. Delivery studies showed "burst" release within 4 h, after that it was slower yielding ~70% of released drug within 80 h. Proposed nanocarriers supported low toxicity against human cells (NHDF and BEAS-2B), anti-inflammation activity evaluated with the use of pro-inflammatory interleukins (IL-6 and IL-8) and antibacterial activities towards E. coli. Adjustment of ionic drug content by structural parameters of graft copolymers, including grafting degree and graft length, are advantageous to tailor nanocarriers with self-assembly properties in aqueous media. Effective release process by ionic exchange and biological activity with low toxicity are promising for further development of this type of drug delivery (DDS).

摘要

基于接枝聚离子液体的新型载体被设计用于输送离子键合的水杨酸盐(Sal)。通过可控自由基聚合,成功地在侧链中以各种含量引入了胆碱衍生的离子液体单体单元。通过侧链的适当长度和接枝度,可以在聚合物体系中实现适当高含量的离子药物。在水溶液中,接枝共聚物自组装成高达 73nm 的球形超结构。递送研究表明,在 4 小时内会出现“突释”,之后释放速度较慢,80 小时内释放约 70%的药物。所提出的纳米载体对人细胞(NHDF 和 BEAS-2B)的毒性较低,通过使用促炎细胞因子(IL-6 和 IL-8)评估其抗炎活性,以及对大肠杆菌的抗菌活性。通过接枝共聚物的结构参数(包括接枝度和接枝长度)来调整离子药物的含量,有利于在水介质中定制具有自组装特性的纳米载体。通过离子交换的有效释放过程和低毒性的生物活性,为这种药物传递(DDS)的进一步发展提供了前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/58a5/6783615/447c48434c4a/41598_2019_50896_Fig1_HTML.jpg

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