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Reactive Oxygen Species-Responsive Liposomes via Boronate-Caged Phosphatidylethanolamine.
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2020-08-18 , DOI: 10.1021/acs.bioconjchem.0c00397 Jinchao Lou 1 , Michael D Best 1
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2020-08-18 , DOI: 10.1021/acs.bioconjchem.0c00397 Jinchao Lou 1 , Michael D Best 1
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Liposomes have proven to be effective nanocarriers due to their ability to encapsulate and deliver a wide variety of therapeutic cargo. A key goal of liposome research is to enhance control over content release at diseased sites. Though a number of stimuli have been explored for triggering liposomal release, reactive oxygen species (ROS), which have received significantly less attention, provide excellent targets due to their key roles in biology and overabundance in diseased cells. Here, we report a ROS-responsive liposome platform through the inclusion of lipid 1 bearing a boronate ester headgroup and a quinone-methide (QM) generating self-immolative linker attached onto a dioleoylphosphatidylethanolamine (DOPE) lipid scaffold. Fluorescence-based dye release assays validated that this system enables release of both hydrophobic and hydrophilic contents upon hydrogen peroxide (H2O2) addition. Details of the release process were carefully studied, and data showed that oxidative removal of the boronate headgroup is sufficient to result in hydrophobic content release, while production of DOPE is needed for hydrophilic cargo leakage. These results showcase that lipid 1 can serve as a promising ROS-responsive liposomal delivery platform for controlled release.
中文翻译：
通过硼酸盐笼蔽的磷脂酰乙醇胺的活性氧反应型脂质体。
脂质体由于其封装和递送多种治疗药物的能力而被证明是有效的纳米载体。脂质体研究的关键目标是增强对患病部位内容物释放的控制。尽管已经探索了许多刺激来触发脂质体释放，但是活性氧（ROS）由于其在生物学中的关键作用以及在患病细胞中的丰度，因此受到了较少的关注，它们提供了出色的靶标。在这里，我们报告通过脂质1的包含一个ROS反应脂质体平台带有硼酸酯头基和醌-甲基（QM）生成自消灭性连接器，该连接器连接到油酰磷脂酰乙醇胺（DOPE）脂质支架上。基于荧光的染料释放分析验证了该系统能够在添加过氧化氢（H 2 O 2）时释放疏水性和亲水性成分。仔细研究了释放过程的细节，数据表明，硼酸酯头基的氧化去除足以导致疏水性内容物释放，而亲水性货物泄漏需要DOPE的产生。这些结果表明脂质1可以作为有希望的ROS响应脂质体传递平台进行控释。
更新日期：2020-09-16
中文翻译：
通过硼酸盐笼蔽的磷脂酰乙醇胺的活性氧反应型脂质体。
脂质体由于其封装和递送多种治疗药物的能力而被证明是有效的纳米载体。脂质体研究的关键目标是增强对患病部位内容物释放的控制。尽管已经探索了许多刺激来触发脂质体释放，但是活性氧（ROS）由于其在生物学中的关键作用以及在患病细胞中的丰度，因此受到了较少的关注，它们提供了出色的靶标。在这里，我们报告通过脂质1的包含一个ROS反应脂质体平台带有硼酸酯头基和醌-甲基（QM）生成自消灭性连接器，该连接器连接到油酰磷脂酰乙醇胺（DOPE）脂质支架上。基于荧光的染料释放分析验证了该系统能够在添加过氧化氢（H 2 O 2）时释放疏水性和亲水性成分。仔细研究了释放过程的细节，数据表明，硼酸酯头基的氧化去除足以导致疏水性内容物释放，而亲水性货物泄漏需要DOPE的产生。这些结果表明脂质1可以作为有希望的ROS响应脂质体传递平台进行控释。
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