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靶向中性粒细胞/单核细胞的双配体修饰脂质体递送葛根素用于缺血性中风治疗

Neutrophil/monocyte-targeted dual-ligands modified liposomes delivering puerarin for ischemia stroke treatment.

作者信息

Ling Chengli, Chen Linglong, Liang Jianming, Li Xiaofang, Wei Hua, Yu Cuiyun, Wang Jianxin

机构信息

Department of Pharmaceutics, School of Pharmacy, Fudan University & Key Laboratory of Smart Drug Delivery, Ministry of Education, Shanghai, 201203, PR China.

Hunan Province Hospital of Integrated Traditional Chinese and Western Medicine (Affiliated Hospital of Hunan Academy of Chinese Medicine), Hunan Academy of Chinese Medicine, Changsha, 410006, PR China.

出版信息

Mater Today Bio. 2025 Jul 12;33:102077. doi: 10.1016/j.mtbio.2025.102077. eCollection 2025 Aug.

DOI:10.1016/j.mtbio.2025.102077
PMID:40697323
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12281153/
Abstract

Extremely low actual biological effect of insoluble small molecule drugs in ischemia region is a pain point and aporia in Ischemia Stroke (IS) therapy, Although there are studies on single, double-ligands modified liposomes or biomimetic exogenous carriers for directly targeting IS so far, but they often have off-target effects due to they were swallowed, degraded directly (instability) and sabotaged without the help of endogenous cell in the systemic circulation. DSPE-PEG-PGP (PGP) and DSPE-PEG-cRGD (cRGD) were synthesized via michael addition reaction of maleimide (-Mal) with sulfhydryl (-SH), succinimidyl ester (-NHS) with active primary amine group (-NH) respectively. The cRGD and PGP were modified on liposomes by thin film hydration method. Optimal modified ratio of cRGD and PGP were achieved by cellular uptake of HL-60 cells and THP-1 cells . The precise targeting effects of cRGD/PGP-Lips were examined in a nude MCAO model by an in a vivo imaging system. Puerarin (Pue) was cleverly encapsulated using a calcium acetate gradient to construct cRGD/PGP-Pue-Lips, and its therapeutic efficiency were assessed by rat MCAO model of IS. Optimal modification ratio for both cRGD and PGP were 3 %. The cRGD/PGP-Lips had significant synergetic targeting efficiency and , and the encapsulation efficiency of Pue were greater than 80 % through calcium acetate gradient. The cRGD/PGP-Pue-Lips could effectively penetrate BBB and enhance Pue retention on the brain ischemia region , resulting in a nearly two-fold reduction significantly in cerebral infarction area and edema in rats. In addition, cRGD/PGP-Pue-Lips didn't cause systemic toxicity in major organ tissues. Precise dual-ligands modified nanocarrier targeting endogenous cells is highly competitive as a novel anti-stroke and perspective for treatment of IS.

摘要

难溶性小分子药物在缺血区域极低的实际生物学效应是缺血性中风（IS）治疗中的一个痛点和难题。尽管目前有关于单配体、双配体修饰脂质体或仿生外源性载体直接靶向IS的研究，但它们在体循环中常因被吞噬、直接降解（稳定性差）以及缺乏内源性细胞的帮助而被破坏，从而产生脱靶效应。分别通过马来酰亚胺（-Mal）与巯基（-SH）、琥珀酰亚胺酯（-NHS）与活性伯胺基团（-NH）的迈克尔加成反应合成了二硬脂酰磷脂酰乙醇胺-聚乙二醇-血小板糖蛋白（PGP）和二硬脂酰磷脂酰乙醇胺-聚乙二醇-环磷酰胺（cRGD）。采用薄膜水化法将cRGD和PGP修饰在脂质体上。通过HL-60细胞和THP-1细胞的摄取实现了cRGD和PGP的最佳修饰比例。利用体内成像系统在裸鼠大脑中动脉闭塞（MCAO）模型中检测了cRGD/PGP-脂质体的精确靶向效果。采用醋酸钙梯度法巧妙地包封葛根素（Pue）构建cRGD/PGP-Pue-脂质体，并通过大鼠IS的MCAO模型评估其治疗效果。cRGD和PGP的最佳修饰比例均为3%。cRGD/PGP-脂质体具有显著的协同靶向效率，通过醋酸钙梯度法，Pue的包封率大于80%。cRGD/PGP-Pue-脂质体能够有效穿透血脑屏障并增强Pue在脑缺血区域的滞留，导致大鼠脑梗死面积和水肿显著减少近两倍。此外，cRGD/PGP-Pue-脂质体在主要器官组织中未引起全身毒性。精确的双配体修饰纳米载体靶向内源性细胞作为一种新型抗中风药物，在IS治疗方面具有高度竞争力和前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b97/12281153/03782d052fa4/gr8.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1b97/12281153/29066f4661f1/ga1.jpg
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