Enhanced Anti-tumor of Pep-1 Modified Superparamagnetic Iron Oxide/PTX Loaded Polymer Nanoparticles
Enhanced Anti-tumor of Pep-1 Modified Superparamagnetic Iron Oxide/PTX Loaded Polymer Nanoparticles
复制标题
Pep-1 修饰的超顺磁性氧化铁/PTX 负载聚合物纳米粒子的增强抗肿瘤作用
DOI：
10.3389/fphar.2018.01556
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发表时间：
2019-01-22
影响因子：
5.6
通讯作者：
Xin, Hongliang
中科院分区：
文献类型：
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作者：
Wang, Baoyan;Wu, Weijun;Xin, Hongliang
超顺磁性氧化铁纳米粒子（SPION）由于其独特的性质，在药物传递领域得到了广泛的关注。在本研究中，我们开发了紫杉醇（PTX）和SPION共载PLGA纳米粒，修饰Pep-1肽（Pep-NP-SPION/PTX）的双重靶向给药系统，以实现肿瘤治疗的磁靶向和主动靶向。采用共沉淀法合成SPION，并将其与紫杉醇（PTX）同时包封于PLGA纳米粒中。然后，通过化学修饰将非复合物与Pep-1偶联。所得Pep-NP-SPION/PTX显示球形形态和IOOnm的平均尺寸。通过体外细胞实验证明Pep-NP-SPION的细胞摄取增强。Pep-NP-SPION/PTX和NP-SPION/PTX的IC 50值分别测定为10.2和19.4 μ g/mL。生物分布研究表明，与非靶向纳米复合物相比，Pep-NP-SPION在肿瘤中的蓄积明显更高。此外，在磁场条件下，NP-SPION和Pep-NP-SPION都表现出更高的肿瘤分布。此外，Pep-NP-SPION/PTX基于主动靶向和磁性靶向特性呈现出期望的体内抗肿瘤效果。总之，Pep-NP-SPION/PTX可以提供磁性靶向和受体介导的靶向以增强抗肿瘤结果。
Superparamagnetic iron-oxide nanoparticle (SPION) has gained tremendous attention for drug delivery applications due to their unique properties. In this study, we developed a dual targeted delivery system with paclitaxel (PTX) and SPION co-loaded PLGA nanoparticles, modified with Pep-1 peptide (Pep-NP-SPION/PTX), to achieve magnetic targeting and active targeting for tumor treatment. SPION was synthesized by a co-precipitation method and was then encapsulated with PTX simultaneously into PLGA nanoparticles. After that, the non-complex was conjugated with Pep-1 through chemical modification. The resulting Pep-NP-SPION/PTX showed a spherical morphology and an average size of 100 nm. The enhancement cellular uptake of Pep-NP-SPION was demonstrated in in vitro through cell experiments. The IC50 value of Pep-NP-SPION/PTX and NP-SPION/PTX was determined to be 10.2 and 19.4 mu g/mL, respectively. A biodistribution study showed that obvious higher accumulations of Pep-NP-SPION was observed in tumors, compared with that of non-targeting nanocomposites. Moreover, under the condition of a magnetic field, both NP-SPION and Pep-NP-SPION exhibited much higher tumor distribution. Furthermore, Pep-NP-SPION/PTX presented desirable in vivo anti-tumor effects based on active targeting and magnetic targeting characteristics. Altogether, Pep-NP-SPION/PTX can offer magnetic targeting and receptor mediated targeting to enhance the anti-tumor outcome.