College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
Nanomedicine. 2014 Feb;10(2):349-58. doi: 10.1016/j.nano.2013.08.004. Epub 2013 Aug 20.
Breast cancer remains one of the most common cancers for females. Drug delivery based on cancer nanotechnology could improve the performance of some chemotherapeutic medicines already used in clinic. The emergence of polymersomes provided the potential to encapsulate hydrophobic/hydrophilic drugs. By modifying the weight ratio of methoxy-poly (ethylene glycol) (mPEG) chain to ethyl-p-aminobenzoate (EAB) side group, a series of amphiphilic graft polyphosphazenes (PEPs) was prepared. PEP can be tuned from micelles to polymersomes with the decrease of mPEG content via dialysis. Either hydrophilic doxorubicin hydrochloride (DOX·HCl) or hydrophobic doxorubicin base (DOX) could be encapsulated into PEP polymersomes with high payload and high encapsulation efficiency due to the strong intermolecular interaction with PEP. Compared with free DOX·HCl administration, in vivo investigation in growth inhibition of MCF-7 xenograft tumors in nude mice demonstrated that PEP polymersomes could enhance life safety without compromise of therapeutic efficacy, especially DOX·HCl loaded delivery system.
In this preclinical study, polymerosomes based on PEPs were investigated as doxorubicin delivery systems, demonstrating similar efficacy but less toxicity compared to standard delivery methods.
乳腺癌仍然是女性最常见的癌症之一。基于癌症纳米技术的药物输送可以提高一些已经在临床上使用的化疗药物的性能。聚合物囊泡的出现提供了封装疏水性/亲水性药物的潜力。通过改变甲氧基聚（乙二醇）（mPEG）链与乙基对氨基苯甲酸酯（EAB）侧基的重量比，制备了一系列两亲性接枝聚膦腈（PEP）。通过透析，随着 mPEG 含量的减少，PEP 可以从胶束调变为聚合物囊泡。由于与 PEP 具有强分子间相互作用，亲水性盐酸多柔比星（DOX·HCl）或疏水性多柔比星碱（DOX）都可以被封装到 PEP 聚合物囊泡中，具有高载药量和高包封效率。与游离 DOX·HCl 给药相比，在裸鼠 MCF-7 异种移植肿瘤生长抑制的体内研究中，PEP 聚合物囊泡可以提高生活安全性而不影响治疗效果，特别是 DOX·HCl 负载的递送系统。
在这项临床前研究中，研究了基于 PEP 的聚合物囊泡作为多柔比星的递送系统，与标准递送方法相比，表现出相似的疗效，但毒性更小。
