Atherosclerosis is a chronic disease that can lead to life‐threatening events such as myocardial infarction and stroke, is characterized by the build‐up of lipids and immune cells within the arterial wall. It is understood that inflammation is a hallmark of atherosclerosis and can be a target for therapy. In support of this concept, an injectable nanoliposomal formulation encapsulating fluocinolone acetonide (FA), a corticosteroid, is developed that allows for drug delivery to atherosclerotic plaques while reducing the systemic exposure to off‐target tissues. In this study, FA is successfully incorporated into liposomal nanocarriers of around 100 nm in size with loading efficiency of 90% and the formulation exhibits sustained release up to 25 d. The anti‐inflammatory effect and cholesterol efflux capability of FA‐liposomes are demonstrated in vitro. In vivo studies carried out with an apolipoprotein E‐knockout (Apoe^−/−) mouse model of atherosclerosis show accumulation of liposomes in atherosclerotic plaques, colocalization with plaque macrophages and anti‐atherogenic effect over 3 weeks of treatment. This FA‐liposomal‐based nanocarrier represents a novel potent nanotherapeutic option for atherosclerosis.

中文翻译：

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脂质体纳米疗法治疗动脉粥样硬化。

动脉粥样硬化是一种慢性疾病，可导致危及生命的事件，例如心肌梗塞和中风，其特征是动脉壁内脂质和免疫细胞的积累。可以理解，炎症是动脉粥样硬化的标志，可以作为治疗的目标。为了支持这一概念，开发了一种可注射的纳米脂质体制剂，其中包封了一种皮质类固醇氟轻松（FA），可将药物递送至动脉粥样硬化斑块，同时减少全身暴露于脱靶组织的风险。在这项研究中，FA成功地掺入了大小约为100 nm的脂质体纳米载体中，负载效率为90％，并且该制剂在长达25 d的时间内表现出持续释放。FA脂质体的抗炎作用和胆固醇外排能力已在体外证明。用载脂蛋白E基因敲除（Apoe^-/-）动脉粥样硬化小鼠模型显示，脂质体在动脉粥样硬化斑块中积累，与斑块巨噬细胞共定位并在治疗3周内具有抗动脉粥样硬化作用。这种基于FA脂质体的纳米载体代表了动脉粥样硬化的一种新型有效的纳米治疗选择。