Department of Polymer Science and Engineering, Key Laboratory of Systems Bioengineering (Ministry of Education), School of Chemical Engineering and Technology, Tianjin University, Tianjin, 300072, China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin, 300072, China.
Macromol Biosci. 2018 Jul;18(7):e1800049. doi: 10.1002/mabi.201800049. Epub 2018 May 7.
Liposomes have shown great promises for pharmaceutical applications, but still suffer from the poor storage stability, undesirable drug leakage, and uncontrolled drug release. Herein, liposomes-camouflaged redox-responsive nanogels platform (denoted as "R-lipogels") is prepared to integrate the desirable features of sensitive nanogels into liposomes to circumvent their intrinsic issues. The results indicate that drug-loaded R-lipogels with controlled size and high stability not only can achieve a very high doxorubicin (DOX)-loading capacity (12.9%) and encapsulation efficiency (97.3%) by ammonium sulfate gradient method and very low premature leakage at physiological condition, but also can quickly release DOX in the reducing microenvironment of tumor cells, resulting in effective growth inhibition of tumor cells. In summary, the strategy given here provides a facile approach to develop liposomes-nanogels hybrid system with combined beneficial features of stealthy liposomes and responsive nanogels, which potentially resolves the dilemma between systemic stability and intracellular rapid drug release.
脂质体在药物应用方面显示出巨大的前景，但仍存在储存稳定性差、药物泄漏不理想和药物释放不可控等问题。本文制备了脂质体伪装的氧化还原响应纳米凝胶平台（表示为“R-脂质体”），将敏感纳米凝胶的理想特性集成到脂质体中，以规避其内在问题。结果表明，载药的 R-脂质体具有可控的尺寸和高稳定性，不仅可以通过硫酸铵梯度法实现非常高的阿霉素（DOX）载药量（12.9%）和包封效率（97.3%），而且可以在生理条件下非常低的提前泄漏，而且可以在肿瘤细胞的还原微环境中快速释放 DOX，从而有效抑制肿瘤细胞的生长。总之，这里提出的策略为开发具有隐形脂质体和响应性纳米凝胶的联合有益特性的脂质体-纳米凝胶混合系统提供了一种简便的方法，有可能解决系统稳定性和细胞内快速药物释放之间的困境。
