ABSTRACT

Background

Hybrid vesicular systems (lipopolymersomes) are promising platforms for minimizing the liposomes and polymersomes disadvantages in terms of chemotherapeutic transportation. In this regard, lipopolymersome has been designed to integrate the advantage of both polymersomes and liposomes to enable better structural integrity of the bilayer after encapsulation of hydrophobic drugs while maintaining the soft nature of liposomes, superior serum stability, and high encapsulation efficiency of cargos in the bilayer segment.

Research design and Methods

In the present study, we reported preparation and characterization of five camptothecin (CPT)-loaded lipopolymersomal formulations composed of poly (ethylene glycol)–poly (lactic acid) (PEG-PLA) and dipalmitoylphosphatidylcholine (DPPC) at different molar ratios using film rehydration method. Afterward, the preferred formulation was tagged with AS1411 DNA aptamer in order to evaluate the therapeutic index using nucleolin-positive colon cancer cell lines (HT29 and C26).

Results

The obtained data indicated that the prepared CPT-loaded lipopolymersome at a PEG-PLA: DPPC ratio of 75:25 exhibited superior stability and high loading capacity compared to other systems. Moreover, high cytotoxicity of the aptamer-targeted lipopolymersome and increased tumor accumulation were observed in comparison with non-targeted one.

Conclusions

The designed polymer-rich lipopolymersomal platform offers bright future for the development of potent nanomedicine against cancer.

中文翻译：

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制备多功能靶向脂质体，以提高喜树碱在体外和体内对抗结肠腺癌的功效

摘要

背景

混合囊泡系统（脂质体）是减少脂质体和聚合物体在化疗运输方面的缺点的有前途的平台。在这方面，脂质体的设计旨在整合聚合物体和脂质体的优点，使疏水性药物包封后双层结构更加完整，同时保持脂质体的柔软性、优异的血清稳定性和高包封率。双层段。

研究设计和方法

在本研究中，我们报告了五种负载喜树碱 (CPT) 的脂质聚合物制剂的制备和表征，这些制剂由不同摩尔比的聚（乙二醇）-聚（乳酸）（PEG-PLA）和二棕榈酰磷脂酰胆碱（DPPC）组成，使用薄膜再水化方法。之后，优选的制剂用 AS1411 DNA 适体标记，以便使用核仁蛋白阳性结肠癌细胞系（HT29 和 C26）评估治疗指数。

结果

获得的数据表明，与其他系统相比，制备的 PEG-PLA:DPPC 比率为 75:25 的 CPT 负载脂质体表现出优异的稳定性和高负载能力。此外，与非靶向脂质体相比，适体靶向脂质体的高细胞毒性和肿瘤积累增加。

结论

设计的富含聚合物的脂质体平台为开发有效的抗癌纳米药物提供了光明的未来。