文献：Berberin sustained-release nanoparticles were enriched in infarcted rat myocardium and resolved inflammation

文献链接：https://link.springer.com/article/10.1186/s12951-023-01790-w

作者：Ke Zhu , Yu Yao , Kun Wang , Fuqiang Shao , Ziyang Zhu , Yangmeihui Song , Zhangyongxue Zhou , Dawei Jiang , Xiaoli Lan , Chunxia Qin

相关产品：DSPE-PEG -Cy7（磷脂-聚乙二醇2000-CY7）

原文摘要：

Inflammatory regulation induced by macrophage polarization is essential for cardiac repair after myocardial infarction (MI). Berberin (BBR) is an isoquinoline tetrasystemic alkaloid extracted from plants. This study analyzes the most likely mechanism of BBR in MI treatment determined via network pharmacology, showing that BBR acts mainly through inflammatory responses. Because platelets (PLTs) can be enriched in the infarcted myocardium, PLT membrane-coated polylactic-co-glycolic acid (PLGA) nanoparticles (BBR@PLGA@PLT NPs) are used, which show enrichment in the infarcted myocardium to deliver BBR sustainably. Compared with PLGA nanoparticles, BBR@PLGA@PLT NPs are more enriched in the infarcted myocardium and exhibit less uptake in the liver. On day three after MI, BBR@PLGA@PLT NPs administration significantly increases the number of repaired macrophages and decreases the number of inflammatory macrophages and apoptotic cells in infarcted rat myocardium. On the 28th day after MI, the BBR@PLGA@PLT group exhibits a protective effect on cardiac function, reduced cardiac collagen deposition, improved scar tissue stiffness, and an excellent angiogenesis effect. In addition, BBR@PLGA@PLT group has no significant impact on major organs either histologically or enzymologically. In summary, the therapeutic effect of BBR@PLGA@PLT NPs on MI is presented in detail from the perspective of the resolution of inflammation, and a new solution for MI treatment is proposed.   

DSPE-PEG 2000 -Cy7：DSPE - PEG2000 - Cy7 是一种具有多种功能的化合物。DSPE 代表 1,2 -二硬脂酰-磷脂酰乙醇胺（1,2 - Distearoyl- sn - Glycero - 3 - Phosphoethanolamine），它是一种磷脂成分。PEG2000 是聚乙二醇（Polyethylene Glycol），其分子量约为 2000 道尔顿，聚乙二醇具有良好的水溶性和生物相容性。Cy7 是一种近红外荧光染料（Cyanine 7），发射波长在近红外区域（大约 750 - 770nm）。基于DSPE-PEG 2000 -Cy7 的性能，该文献介绍如下：

图：机制流程示意

BBR@PLGA@PLT NPs的制备：

用二氯甲烷溶解PLGA，将新制备的小檗碱溶液加入到PLGA溶液中。然后使用探针超声仪在冰浴中对混合物进行超声，在一定振幅下交替开关。将混合物（W1/O）快速加入 PVA1788 溶液中，以一定的速度在冰浴（W1/O/W2）中高速均质。将悬浊液加入异丙醇；用磁力搅拌器在搅拌下过夜，去除剩余的二氯甲烷。BBR@PLGA用去离子水离心洗涤。最后，BBR@PLGA冻干，装入密封的青霉素瓶中。将platelets ghosts的分散体浴声器中超声，以完成细胞膜涂层。将含可吸入颗粒的去离子水与全血中的PLT  ghosts混合。二硬脂酰磷脂酰乙醇胺（DSPE）作为一种疏水性基团，具有良好的生物可扩展性，可嵌入血小板膜中。因此，采用DSPE-PEG2000-Cy7荧光标记BBR@PLGA@PLT。

图：表征图像

结论：

该文献成功制备出纳米粒子BBR@PLGA@PLT NPs，并用DSPE-PEG 2000 -Cy7 标记。研究发现，BBR@PLGA@PLT NPs可以保护心肌功能，减少心脏不良重构，维持心肌组织结构完整性，保护心肌细胞，通过解决心肌Inflammation促进梗死心肌Blood vessels生成。DSPE-PEG 2000 -Cy7 在实验过程中起到很好的标记成像作用。