Superhydrophilic Zwitterionic Polymers Stabilize Liposomes
Superhydrophilic Zwitterionic Polymers Stabilize Liposomes
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DOI：
10.1021/la302433a
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发表时间：
2012-08-07
期刊：
影响因子：
3.9
通讯作者：
Jiang, Shaoyi
中科院分区：
文献类型：
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作者：
Cao, Zhiqiang;Zhang, Lei;Jiang, Shaoyi
非离子聚乙二醇（PEG）作为一种隐形聚合物，由于其两亲性，会使脂质体不稳定。因此，必须进一步稳定PEG化脂质体，例如通过使用大量胆固醇。这是PEG面临的一个长期存在的困境。在这项工作中，我们表明，两性离子聚（羧基甜菜碱）（PCB）稳定脂质体，因为它的超亲水性，从而解决了这个难题，具体地说，PCB修饰的脂质体没有胆固醇表现出良好的保留亲水性药物和长的血液循环特性在体内。为了进一步验证这种新的PCB化学，将不含胆固醇的PCB脂质体多柔比星与DOXIL的抗肿瘤治疗功效进行了比较。
Nonionic polyethylene glycol (PEG) as a stealth polymer destabilizes liposomes due to its amphiphilic property. As a result, PEGylated liposomes have to be further stabilized, such as by using a large amount cholesterol. This is a long existing dilemma faced by PEG. In this work, we show that zwitterionic poly(carboxybetaine) (PCB) stabilizes liposomes because of its superhydrophilic nature, thus solving this dilemma, Specifically, PCB-modified liposomes without cholesterol exhibited good retention of hydrophilic drug and long blood circulating characteristics in vivo. To further validate this new PCB chemistry, PCB liposomal doxorubicin without cholesterol was compared with DOXIL for their antitumor therapeutic efficacies.