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Emulsions of hydrolyzable oils for the zero-order release of hydrophobic drugs
Journal of Controlled Release ( IF 10.8 ) Pub Date : 2021-10-15 , DOI: 10.1016/j.jconrel.2021.10.014
Laura Tebcharani 1 , Caren Wanzke 1 , Theresa M Lutz 2 , Jennifer Rodon-Fores 1 , Oliver Lieleg 2 , Job Boekhoven 1
Affiliation  

Drug delivery systems that release hydrophobic drugs with zero-order kinetics remain rare and are often complicated to use. In this work, we present a gellified emulsion (emulgel) that comprises oil droplets of a hydrolyzable oil entrapped in a hydrogel. In the oil, we incorporate various hydrophobic drugs and, because the oil hydrolyzes with zero-order kinetics, the release of the drugs is also linear. We tune the release period from three hours to 50 h by varying the initial oil concentration. We show that the release rate is tunable by varying the initial drug concentration. Our quantitative understanding of the system allows for predicting the drug release kinetics once the drug's partition coefficient between the oil and the aqueous phase is known. Finally, we show that our drug delivery system is fully functional after storing it at −20 °C. Cell viability studies show that the hydrolyzable oil and its hydrolysis product are non-toxic under the employed conditions. With its simplicity and versatility, our system is a promising platform for the zero-order release of the drug.



中文翻译:

用于疏水性药物零级释放的可水解油乳液

以零级动力学释放疏水性药物的给药系统仍然很少见,而且使用起来往往很复杂。在这项工作中,我们提出了一种凝胶化的乳液(乳液),它包含包裹在水凝胶中的可水解油的油滴。在油中,我们加入了各种疏水性药物,因为油以零级动力学水解,药物的释放也是线性的。我们通过改变初始油浓度将释放时间从 3 小时调整到 50 小时。我们表明通过改变初始药物浓度可以调节释放速率。一旦已知药物在油相和水相之间的分配系数,我们对系统的定量理解允许预测药物释放动力学。最后,我们表明,我们的给药系统在 -20 °C 下储存后功能齐全。细胞活力研究表明,可水解油及其水解产物在所采用的条件下是无毒的。凭借其简单性和多功能性,我们的系统是药物零级释放的有前途的平台。

更新日期:2021-10-22
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