Lucía Martín-Navarro, Lucía Martín-Banderas, María Dolores Herrera
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引用次数: 0
摘要
为了有选择性地向动脉粥样硬化斑块输送大麻素药物(CB2 激动剂),我们获得了生物相容性和可生物降解的纳米颗粒。为此,PEG 化纳米粒子被一种肽功能化,该肽能够选择性地与动脉粥样硬化斑块中过度表达的内皮粘附蛋白(血管细胞粘附分子 1,VCAM-1)结合。这种微粒在理化、体外细胞培养和体内动脉粥样硬化动物模型(缺乏载脂蛋白 E 的载脂蛋白 E-/- 小鼠)中均有表征,显示出最佳的大麻素释放时空控制和卓越的药理反应。鉴于 CB2 激动剂药物具有高亲脂性和低可用性,采用选择性纳米系统来载体化这些抗动脉粥样硬化药物将提高其生物利用度和疗效。此次展示的工作是之前一个项目的部分成果。这些成果为我们获得新的资助提供了支持,以解决涉及引入诊断元素和植物大麻素的更先进战略问题。
Active cannabinoid nanocarriers for the treatment of atherosclerosis
In order to selectively deliver cannabinoid drugs (CB2 agonists) to the atherosclerotic plaque, biocompatible and biodegradable nanoparticles have been obtained. For this purpose, the PEGylated nanoparticles have been functionalized with a peptide capable of selectively binding to endothelial adhesion proteins overexpressed in the atherosclerotic plaque (vascular cell adhesion molecules 1, VCAM-1). The particles have been characterized physicochemically, in vitro in cell cultures and in vivo in an animal model of atherosclerosis (apolipoprotein E-deficient ApoE-/- mice), demonstrating optimal spatiotemporal control of cannabinoid release and superior pharmacological response. Given that CB2 agonist drugs present high lipophilicity and low availability, the introduction of selective nanosystems for the vehiculation of these antiatherogenic drugs would improve their bioavailability and efficacy. The work presented shows part of the results obtained from a previous project. These results have supported us for the award of a new funding grant to address a more advanced strategy involving the introduction of diagnostic elements and a phytocannabinoid.
期刊介绍:
The Anales de la Real Academia Nacional de Farmacia� embraces all aspects of pharmaceutical sciences and is a quarterly journal that publishes basic and applied research on pharmaceutical sciences and related areas. It is a medium for reporting selected original and significant contributions to new pharmaceutical knowledge.