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Clickable Cubosomes for Antibody-Free Drug Targeting and Imaging Applications
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-12-20 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00659 Nicolas Alcaraz 1, 2 , Qingtao Liu 1, 2 , Eric Hanssen 3 , Angus Johnston 1, 2 , Ben J. Boyd 1, 2
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-12-20 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00659 Nicolas Alcaraz 1, 2 , Qingtao Liu 1, 2 , Eric Hanssen 3 , Angus Johnston 1, 2 , Ben J. Boyd 1, 2
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The combination of copper-free click chemistry with metabolic labeling offers new opportunities in drug delivery. The objective of this study was to determine whether cubosomes functionalized with azide or dibenzocyclooctyne (DBCO) groups are able to undergo copper-free click chemistry with a strained cyclooctyne or azide, respectively. Phytantriol-based cubosomes were functionalized using phospholipids bearing an azide or DBCO group. The modified cubosome dispersions were characterized using dynamic light scattering, cryo-TEM, and small-angle X-ray scattering. The efficiency of “clickability” was assessed by reacting the cubosomes with a complementary dye and determining bound and unbound dye via size exclusion chromatography. The clickable cubosomes reacted specifically and efficiently with a click-Cy5 dye with minor changes to the size, shape, and structure of the cubosomes. This indicates that cubosomes can retain their unique internal structure while participating in copper-free click chemistry. This proof of concept study paves the way for the use of copper-free click chemistry and metabolic labeling with cubosomes for targeted drug delivery and imaging.
中文翻译：
可点击的立方小体，用于无抗体的药物靶向和成像应用
无铜点击化学与代谢标记的结合为药物输送提供了新的机会。这项研究的目的是确定用叠氮化物或二苯并环辛炔（DBCO）基团官能化的立方微粒是否能够分别通过应变的辛烯或叠氮化物进行无铜点击化学反应。使用带有叠氮化物或DBCO基团的磷脂对基于植物三醇的立方脂质体进行功能化。使用动态光散射，低温TEM和小角X射线散射对改性的立方微粒分散体进行表征。通过使立方体与互补染料反应，并通过尺寸排阻色谱法确定结合和未结合的染料，来评估“可点击性”的效率。可点击的立方小体与点击-Cy5染料发生了特异性和有效的反应，但其大小，形状，和立方体的结构。这表明立方脂质体在参与无铜点击化学过程中可以保留其独特的内部结构。这项概念验证研究为将无铜点击化学和代谢标记与立方脂质体用于靶向药物递送和成像铺平了道路。
更新日期：2017-12-20
中文翻译：
可点击的立方小体，用于无抗体的药物靶向和成像应用
无铜点击化学与代谢标记的结合为药物输送提供了新的机会。这项研究的目的是确定用叠氮化物或二苯并环辛炔（DBCO）基团官能化的立方微粒是否能够分别通过应变的辛烯或叠氮化物进行无铜点击化学反应。使用带有叠氮化物或DBCO基团的磷脂对基于植物三醇的立方脂质体进行功能化。使用动态光散射，低温TEM和小角X射线散射对改性的立方微粒分散体进行表征。通过使立方体与互补染料反应，并通过尺寸排阻色谱法确定结合和未结合的染料，来评估“可点击性”的效率。可点击的立方小体与点击-Cy5染料发生了特异性和有效的反应，但其大小，形状，和立方体的结构。这表明立方脂质体在参与无铜点击化学过程中可以保留其独特的内部结构。这项概念验证研究为将无铜点击化学和代谢标记与立方脂质体用于靶向药物递送和成像铺平了道路。
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