Department of Chemistry, M.V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation,
Int J Nanomedicine. 2019 Feb 8;14:1039-1049. doi: 10.2147/IJN.S190306. eCollection 2019.
Nowadays, the development of stimuli-sensitive nanocontainers for targeted drug delivery is of great value. Encapsulation of a drug in a pH-sensitive liposomal container not only provides protective and transport functions, but also helps to create a system with a controlled release mechanism.
In this study, we investigated the influence of a cationic polypeptide on the pH-induced release of anticancer drug doxorubicin (DXR) from the anionic fliposomes - liposomes consisting of a neutral lipid, an anionic lipid (prone to interact with a polycation), and a lipid trigger (imparting the pH-sensitivity).
First, we showed the possibility to control the pH-induced release by the simple modification of the anionic fliposomes with linear polylysine. Second, we optimized the fliposomal composition such that the obtained fliposomes responded to the pH changes only when complexed with the polycation ("turning on" the release). Finally, pH-induced release from the polylysine-modified anionic fliposomes was tested on an anticancer drug DXR.
We have succeeded in developing "smart" stimuli-sensitive nanocontainers capable of tunable controlled release of a drug. Moreover, based on the data on release of a low molecular salt, one can predict the release profile of DXR.
如今，开发用于靶向药物递送的刺激敏感纳米容器具有重要价值。将药物封装在 pH 敏感的脂质体容器中不仅提供了保护和运输功能，还有助于创建具有控制释放机制的系统。
在这项研究中，我们研究了阳离子多肽对阿霉素（DXR）从阴离子翻转体（由中性脂质、阴离子脂质（易于与聚阳离子相互作用）和脂质触发剂（赋予 pH 敏感性）组成的脂质体）的 pH 诱导释放的影响。
首先，我们通过简单地用线性多聚赖氨酸修饰阴离子翻转体，展示了控制 pH 诱导释放的可能性。其次，我们优化了翻转体的组成，使得只有在与聚阳离子复合时，才能对 pH 变化做出反应（“开启”释放）。最后，在抗癌药物 DXR 上测试了聚赖氨酸修饰的阴离子翻转体的 pH 诱导释放。
我们已经成功开发出能够实现可调控制释放药物的“智能”刺激敏感纳米容器。此外，基于对小分子盐释放的数据，可以预测 DXR 的释放曲线。
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