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载磁铁矿的含氟聚合物胶束用于磁共振成像和药物递送。

Magnetite-loaded fluorine-containing polymeric micelles for magnetic resonance imaging and drug delivery.

机构信息

Ministry of Education Key Laboratory for the Green Preparation and Application of Functional Materials, Hubei University, Wuhan, Hubei 430062, China.

出版信息

Biomaterials. 2012 Apr;33(10):3013-24. doi: 10.1016/j.biomaterials.2011.12.042. Epub 2012 Jan 13.

DOI:10.1016/j.biomaterials.2011.12.042
PMID:22243798
Abstract

Magnetite (Fe(3)O(4)) - loaded polymer micelles (denoted as "magnetomicelles") are produced by self-assembly of fluorine-containing amphiphilic poly(HFMA-g-PEGMA) copolymers with oleic acid modified Fe(3)O(4) nanoparticles in an aqueous medium. The oleic acid modified Fe(3)O(4) nanoparticles form small clusters in the poly(HFMA-g-PEGMA) micelles with a mean diameter of 100 nm and the magnetomicelles show high stability in an aqueous medium due to the high hydrophobic fluorine segments in graft copolymers enhance the stability of the micelles. The magnetomicelles also show good cytocompatibility based on the MTT cytotoxicity assay and possess paramagnetic properties with saturation magnetization of 17.14 emu/g.Their good stability, cytocompatibility, and paramagnetic properties render the materials attractive in drug delivery and in vivo magnetic resonance imaging (MRI) applications. Controlled release of hydrophobic drug-5-fluorouracil is achieved from the magnetomicelles with a loading efficiency of 20.94 wt%. The magnetomicelles have transverse relaxivity rates (r(2)) of 134.27 mM(-1) s(-1) and exhibit high efficacy as a negative MRI agent in T(2)-weighted imaging. In vivo MRI studies demonstrate that the contrast between liver and spleen is enhanced by the magnetomicelles. These favorable properties suggest clinical use as nanocarriers in drug delivery applications and contrast agents in MRI.

摘要

载磁铁矿(Fe3O4)聚合物胶束(表示为“磁胶束”)是通过在水介质中自组装含氟两亲性聚(HFMA-g-PEGMA)共聚物与油酸修饰的 Fe3O4 纳米粒子来制备的。油酸修饰的 Fe3O4 纳米粒子在聚(HFMA-g-PEGMA)胶束中形成小簇,平均直径为 100nm,由于接枝共聚物中高疏水性氟段提高了胶束的稳定性,磁胶束在水介质中表现出高稳定性。基于 MTT 细胞毒性试验,磁胶束还表现出良好的细胞相容性,并具有 17.14 emu/g 的饱和磁化强度的顺磁性。其良好的稳定性、细胞相容性和顺磁性使得这些材料在药物输送和体内磁共振成像(MRI)应用中具有吸引力。载药效率为 20.94wt%的疏水性药物 5-氟尿嘧啶从磁胶束中实现了控制释放。磁胶束的横向弛豫率(r2)为 134.27 mM-1s-1,在 T2 加权成像中表现出作为负性 MRI 造影剂的高效性。体内 MRI 研究表明,磁胶束增强了肝和脾之间的对比度。这些有利的性质表明它们可作为药物输送应用中的纳米载体和 MRI 中的造影剂进行临床应用。

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