Abstract

Aims

This study was conducted to evaluate block copolymers containing two different poly(ethyleneimine) (PEI) amounts, as new pH-sensitive micellar delivery systems for doxorubicin.

Methods

Micelles were prepared with block copolymers consisting of poly(2-ethyl-2-oxazoline)-co-poly(ethyleneimine) (PEtOx-co-PEI) and poly(ε-caprolactone) (PCL) as hydrophilic and hydrophobic blocks, respectively. Doxorubicin loading, micelle size, pH-dependent drug release, and in vitro cytotoxicity on MCF-7 cells were investigated.

Results

The average size of drug-loaded micelles was under 100 nm and drug loading was between 10.7% and 48.3% (w/w). pH-sensitive drug release was more pronounced (84.7% and 68.9% (w/w) of drug was released at pH 5.0 and pH 7.4, respectively) for the micelles of the copolymer with the lowest PEI amount. The cell viability of doxorubicin-loaded micelles which were prepared by the copolymer with the lowest PEI amount was 28–33% at 72 h.

Conclusions

PEtOx-co-PEI-b-PCL micelles of this copolymer were found to be stable and effective pH-sensitive nano-sized carriers for doxorubicin delivery.

中文翻译：

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利用PEtOx-co-PEI的可电离性质制备pH敏感的阿霉素负载胶束。

摘要

目的

进行这项研究以评估含有两种不同聚（乙烯亚胺）（PEI）量的嵌段共聚物，作为新的pH敏感的阿霉素胶束递送系统。

方法

用分别由聚（2-乙基-2-恶唑啉）-共-聚（乙烯亚胺）（PEtOx-共-PEI）和聚（ε-己内酯）（PCL）组成的嵌段共聚物作为亲水性和疏水性嵌段制备胶束。研究了阿霉素的负载量，胶束大小，pH依赖性药物释放以及对MCF-7细胞的体外细胞毒性。

结果

载药胶束的平均尺寸在100 nm以下，载药量在10.7％至48.3％（w / w）之间。对于具有最低PEI量的共聚物胶束，pH敏感的药物释放更为显着（分别在pH 5.0和pH 7.4时释放的药物分别为84.7％和68.9％（w / w））。用最低PEI量的共聚物制备的阿霉素负载胶束在72小时内的细胞活力为28-33％。

结论

发现该共聚物的PEtOx- co- PEI- b- PCL胶束是稳定且有效的pH敏感纳米尺寸载体，可用于阿霉素的递送。