Poly(2-oxazoline) block copolymer nanoparticles for curcumin loading and delivery to cancer cells
Poly(2-oxazoline) block copolymer nanoparticles for curcumin loading and delivery to cancer cells
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用于装载姜黄素并递送至癌细胞的聚（2-恶唑啉）嵌段共聚物纳米粒子
DOI：
10.1016/j.eurpolymj.2017.02.043
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发表时间：
2017
影响因子：
6
通讯作者：
Tim R. Dargaville
中科院分区：
文献类型：
--
作者：
Radhika Raveendran;K. Mullen;R. Wellard;C. Sharma;R. Hoogenboom;Tim R. Dargaville
从香料姜黄中获得的姜黄素以其抗癌活性而闻名，然而，其作为可行药物的使用受到其低水溶性的阻碍。为了解决这个问题，我们研究了基于聚（2-烷基-2-恶唑啉）（PAOx）的两亲性嵌段共聚物作为可行的纳米载体有效地将姜黄素递送到癌细胞的潜力。通过阳离子开环聚合（CROP）合成了由两种不同比例的疏水性和亲水性PAOx单元组成的嵌段共聚物。嵌段共聚物在水介质中自组装形成的纳米颗粒可以将姜黄素包裹在其疏水核中。这些粒径约为100 nm的姜黄素PAOx纳米粒具有良好的稳定性和提高姜黄素的水溶性。体外释放研究表明，姜黄素从PAOx纳米粒中释放具有pH敏感性。通过纳米颗粒介导的递送实现了对C6胶质瘤细胞的显著细胞毒性，沿着这些细胞中姜黄素的增强的内化。研究还表明，PAOx共聚物的疏水嵌段长度在功能上是重要的。这些系统提供了潜在的临床相关性，作为有前途的纳米载体，能够规避姜黄素的临床局限性。
Curcumin, obtained from spice turmeric, is renowned for its anti-cancer activity, however, its use as a viable drug is impeded by its low aqueous solubility. To address this, we have investigated the potential of amphiphilic block copolymers, based on poly(2-alkyl-2-oxazoline)s (PAOx), as feasible nano-carriers for efficiently delivering curcumin to cancer cells. The block copolymers comprising hydrophobic and hydrophilic PAOx units in two different ratios were synthesized by cationic ring opening polymerization (CROP). The nanoparticles, ensuing from the self-assembly of the block copolymers in aqueous media, could encapsulate curcumin in their hydrophobic core. These curcumin loaded PAOx nanoparticles, of size around 100 nm, exhibited excellent stability and enhancement of aqueous solubility of curcumin.In vitrorelease studies demonstrated a pH-sensitive release of curcumin from the PAOx nanoparticles. Profound cytotoxicity on C6 glioma cells, along with enhanced internalization of curcumin in these cells was achieved by the nanoparticle-mediated delivery. It was also revealed that the length of the hydrophobic block of the PAOx copolymers was functionally important. These systems offer potential clinical relevance as promising nano-carriers capable of circumventing the clinical limitations of curcumin.
影响因子：
4.6
作者：
Luxenhofer, Robert;Han, Yingchao;Schulz, Anita;Tong, Jing;He, Zhijian;Kabanov, Alexander V.;Jordan, Rainer
通讯作者：
Jordan, Rainer
DOI：
10.2217/nnm.10.10
发表时间：
2010-04
期刊：
Nanomedicine (London, England)
影响因子：
--
作者：
Trivedi R;Kompella UB
通讯作者：
Kompella UB