Current challenges in oncology are largely associated with the need to improve the effectiveness of cancer treatment and to reduce drug’s side effects. An effective strategy to cope with these challenges is behind designing and developing drug delivery systems based on smart nanomaterials and approved anticancer drugs. The present study offers a novel and straightforward approach to efficiently load the cisplatin drug into the newly constructed liposome-based nanosystems as well a reliable technique for monitoring this process based on capillary electrophoresis hyphenated with inductively coupled plasma tandem mass spectrometry. The proposed drug-loading methodology comprises liposome formation via a simple ethanol-injection method and propels increased drug encapsulation using tailor-made freeze-thawing or lyophilization-hydration procedures. To optimize liposome generation and drug encapsulation, the effects of dilution medium and liposome composition (types of phospholipids and their percentage ratio) have been investigated in detail. It was shown that modest alterations of the composition of three-component phospholipid liposomes and parameters of the freeze-thawing procedure have a strong impact on the formation of cisplatin–liposome systems. The obtained cisplatin–liposome formulation features a remarkable degree of drug encapsulation, over 100 mg L, and holds promise for further preclinical development as a potent drug-delivery platform.

中文翻译：

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提高顺铂药物在脂质体纳米载体中的负载量

当前肿瘤学面临的挑战很大程度上与提高癌症治疗的有效性和减少药物副作用的需要有关。应对这些挑战的有效策略是设计和开发基于智能纳米材料和已批准的抗癌药物的药物输送系统。本研究提供了一种新颖而直接的方法，可以有效地将顺铂药物加载到新构建的基于脂质体的纳米系统中，以及一种基于毛细管电泳与电感耦合等离子体串联质谱联用的监测这一过程的可靠技术。所提出的药物装载方法包括通过简单的乙醇注射方法形成脂质体，并使用定制的冻融或冻干水合程序促进药物封装增加。为了优化脂质体的生成和药物封装，详细研究了稀释介质和脂质体成分（磷脂的类型及其百分比）的影响。结果表明，三组分磷脂脂质体的组成和冻融程序参数的适度改变对顺铂-脂质体系统的形成有很大影响。所获得的顺铂脂质体制剂具有显着的药物封装度，超过 100 mg/L，有望作为有效的药物输送平台进一步进行临床前开发。