Background

Acute myocardial infarction (AMI) is one of the most common ischemic heart diseases. However, lack of sufficient drug concentrations in the ischemic heart may led to treatment failure. It is urgent for researchers to engineer novel drug delivery systems to enhance the targeted delivery of cardioprotective agents.

Objective

The aim of the present study was to investigate the anti-AMI ability of calycosin (CAL) and tanshinone (TAN) co-loaded mitochondria targeted lipid-polymer hybrid nano-system.

Methods

CAL and TAN combined lipid-polymer hybrid nano-systems were prepared and MTP-131 was conjugated with PEG and modified onto the nanoparticles to achieve MTP-CAL/TAN NS. The physicochemical properties of nano-systems were characterized, the AMI therapy ability of the systems was investigated in AMI rats’ model.

Results

The size of MTP-CAL/TAN NS was 168.7 ± 5.1 nm, with a surface charge of − 21.3 ± 2.3 mV. The area under the curve (AUC) and blood circulation half-life (T_1/2) of MTP-CAL/TAN NS was 178.86 ± 6.62 μg·min/mL and 0.47 h, respectively. MTP-CAL/TAN NS exhibited the most significant infarct size reduction effect of 23.9 %.

Conclusion

MTP-CAL/TAN NS exhibited the highest heart accumulation and best infarct size reduction effect, which could be used as a promising system for efficient treatment of cardiovascular diseases.

中文翻译：

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使用毛蕊花素和丹参酮共载线粒体靶向脂质-聚合物杂化纳米系统治疗急性心肌梗死：制备、表征和抗心肌梗死活性评估

背景

急性心肌梗死（AMI）是最常见的缺血性心脏病之一。然而，缺血心脏中缺乏足够的药物浓度可能导致治疗失败。研究人员迫切需要设计新型药物输送系统，以增强心脏保护剂的靶向输送。

客观的

本研究的目的是研究毛囊素 (CAL) 和丹参酮 (TAN) 共载线粒体靶向脂质-聚合物杂化纳米系统的抗 AMI 能力。

方法

制备了 CAL 和 TAN 组合的脂质-聚合物杂化纳米系统，并将 MTP-131 与 PEG 缀合并修饰到纳米颗粒上以实现 MTP-CAL/TAN NS。表征了纳米系统的物理化学性质，并在AMI大鼠模型中研究了该系统的AMI治疗能力。

结果

MTP-CAL/TAN NS 的大小为 168.7 ± 5.1 nm，表面电荷为 − 21.3 ± 2.3 mV。MTP-CAL/TAN NS的曲线下面积（AUC）和血液循环半衰期（T _1/2）分别为178.86 ± 6.62 μg·min/mL和0.47 h。MTP-CAL/TAN NS 表现出最显着的梗塞面积缩小效果，为 23.9%。

结论

MTP-CAL/TAN NS 表现出最高的心脏积累和最佳的梗塞面积缩小效果，可用作有效治疗心血管疾病的有前途的系统。