Engineering magnetic-molecular sequential targeting nanoparticles for anti-cancer therapy.
Engineering magnetic-molecular sequential targeting nanoparticles for anti-cancer therapy.
复制标题
DOI：
10.1039/c3tb20715c
复制
发表时间：
2013-11
期刊：
影响因子：
--
通讯作者：
Qi Zhang;Jundong Zhu;Lichao Song;Ju Zhang;D. Kong;Yanjun Zhao;Z. Wang
中科院分区：
文献类型：
--
作者：
Qi Zhang;Jundong Zhu;Lichao Song;Ju Zhang;D. Kong;Yanjun Zhao;Z. Wang
通过增强渗透性和滞留(EPR)效应向肿瘤传递纳米药物通常受到血液循环和外渗步骤的限制。只有不到10%的给药剂量最终会到达肿瘤组织。为了提高药物的传递效率，我们报道了磁性加分子双靶向纳米粒子将肿瘤靶向、药物传递和原位成像结合在一起的方法。在超顺磁性氧化铁纳米粒子(SPIOns)表面包覆生物相容的聚乙二醇聚乳酸，然后用叶酸(FA)锚定其表面。尽管有FA的存在，SPION的流体动力学尺寸仍小于100 nm。表面FA浓度的增加牺牲了SPION的水溶液稳定性，但20%FA没有引起明显的粒子聚集。20%FA的存在保持了SPION的超顺磁性，饱和磁化强度约为30emu·g-1。含有20%FA的SPION和不含FA的SPION之间的药物释放曲线没有显著差异。然而，当使用MCF-7乳腺癌细胞系时，FA的存在显著增加了SPIOns的细胞内摄取。这些结果突出了表面配体优化在设计所需的磁性-分子双重肿瘤靶向纳米颗粒中的作用。
Nanoparticle drug delivery to tumors via the enhanced permeability and retention (EPR) effect is usually limited by the step of blood circulation and extravasation. Only less than 10% of the administered dose would eventually reach the tumor tissue. To enhance the drug delivery efficiency, we report the approach of magnetic plus molecular dual targeting nanoparticles to combine tumor targeting, drug delivery, and in situ imaging together. The surface of superparamagnetic iron oxide nanoparticles (SPIONs) was coated with biocompatible poly(ethylene glycol)-poly(lactic acid) and then anchored with folic acid (FA). Despite the presence of FA, the hydrodynamic size of SPIONs was less than 100 nm. Increasing the surface FA density sacrificed the aqueous stability of SPIONs, but 20% FA did not induce noticeable particle aggregation. The existence of 20% FA maintained the superparamagnetic property of SPIONs with a saturation magnetization level at ca. 30 emu g-1. The drug release profile was not significantly different between SPIONs with (20%) and without FA. However, the presence of FA dramatically increased the intracellular uptake of SPIONs when using the MCF-7 breast cancer cell line. These results highlighted the role of surface ligand optimization in the design of desired magnetic-molecular dual tumor-targeting nanoparticles.