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急性心肌梗死治疗:评价载黄芩苷的三苯基膦双配体修饰纳米粒系统。

Acute myocardial infarction therapy: and evaluation of atrial natriuretic peptide and triphenylphosphonium dual ligands modified, baicalin-loaded nanoparticulate system.

机构信息

Intervention Center, Linyi People's Hospital Beicheng New District Hospital, Linyi, PR China.

Cardiology Pacing and Electrophysiology Ward, Linyi People's Hospital Beicheng New District Hospital, Linyi, PR China.

出版信息

Drug Deliv. 2021 Dec;28(1):2198-2204. doi: 10.1080/10717544.2021.1989086.

Abstract

BACKGROUND

Myocardial infarction (MI) is one of the most common ischemic heart diseases. It is very essential to explore new types of cardioprotective drugs delivery systems in this area.

OBJECTIVE

The aim of the present study was to investigate the protective effect of baicalin (BA) and puerarin (PU) against acute MI rat models. BA and PU co-loaded nanoparticulate system were developed to improve bioavailability of the drugs, to prolong retention time and to enhance the protective effect.

METHODS

In the present study, ANP and TPP contained ligands were synthesized. ANP/TPP-BN-LPNs were prepared and its physico-chemical properties were evaluated. The MI therapy efficiency of ANP/TPP-BN-LPNs was assessed in rats after intravenous injection. Single ligand contained LPNs, no ligand contained LPNs, and BN solution formulations were also prepared and used for the comparison.

RESULTS

ANP/TPP-BN-LPNs were uniform and spheroidal particles. The size of ANP/TPP-BN-LPNs was 98.5 ± 2.9 nm, with a zeta potential of -19.5 ± 1.9 mV. The dual ligands modified LPNs exhibited significantly improved therapeutic efficiency compared with the single ligand modified LPNs and other systems. infarct therapy studies in rats proved that ANP/TPP-BN-LPNs were a promising system for efficient delivery of cardiovascular drugs for the treatment of cardiovascular diseases.

CONCLUSIONS

ANP/TPP-BN-LPNs could be used as a long-circulating and heart-targeting drug delivery system.

摘要

背景

心肌梗死(MI)是最常见的缺血性心脏病之一。在该领域探索新型心脏保护药物输送系统非常重要。

目的

本研究旨在探讨黄芩苷(BA)和葛根素(PU)对急性心肌梗死大鼠模型的保护作用。开发 BA 和 PU 共载纳米粒系统,以提高药物的生物利用度、延长保留时间并增强保护作用。

方法

在本研究中,合成了含有 ANP 和 TPP 的配体。制备了 ANP/TPP-BN-LPNs,并对其理化性质进行了评价。通过静脉注射后在大鼠体内评估了 ANP/TPP-BN-LPNs 的 MI 治疗效果。还制备了单配体含 LPNs、无配体含 LPNs 和 BN 溶液制剂,并进行了比较。

结果

ANP/TPP-BN-LPNs 为均匀的球形颗粒。ANP/TPP-BN-LPNs 的粒径为 98.5±2.9nm,zeta 电位为-19.5±1.9mV。与单配体修饰的 LPNs 及其他系统相比,双配体修饰的 LPNs 表现出显著改善的治疗效果。大鼠梗死治疗研究证明,ANP/TPP-BN-LPNs 是一种有前途的心血管药物高效递药系统,可用于治疗心血管疾病。

结论

ANP/TPP-BN-LPNs 可作为一种长循环和心脏靶向的药物传递系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8673/8525923/b4d519a0bb91/IDRD_A_1989086_F0001_C.jpg

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