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评价 C60/2-羟丙基-β-环糊精纳米粒的光动力活性。

Evaluation of photodynamic activity of C60/2-hydroxypropyl-β-cyclodextrin nanoparticles.

机构信息

Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto 860-0082, Japan.

出版信息

J Pharm Sci. 2012 Sep;101(9):3390-7. doi: 10.1002/jps.23045. Epub 2012 Jan 6.

DOI:10.1002/jps.23045
PMID:22228093
Abstract

The objective of this study is to evaluate the ability of C(60)/2-hydroxypropyl-β-cyclodextrin (HP-β-CyD) naonparticles to generate reactive oxygen species (ROS) and to induce cell toxicity by the photoirradiation. C(60) nanoparticles were prepared by cogrinding with HP-β-CyD for 3 h at 4°C under reduced pressure. The photodynamic activity of C(60)/HP-β-CyD nanoparticles was evaluated by spectroscopic methods, including the electron spin resonance spin-trapping method, and by the cell viability test using Hela cells. C(60)/HP-β-CyD nanoparticles efficiently generated not only superoxide anion radical (O(2)(·-)) and hydroxyl radical (·OH), but also singlet oxygen ((1)O(2)) through photoirradiation. The ROS generation was enhanced by decreasing the mean particle diameter of C(60) nanoparticles, and the particle size smaller than 90 nm showed a high generation of ·OH and (1)O(2). In addition, HP-β-CyD enhanced the generation of (1)O(2), compared with polyvinylpyrrolidone (an effective solubillizer for C(60)), due to partial disposition of C(60) in the hydrophobic CyD cavity. Furthermore, C(60) /HP-β-CyD nanoparticles showed cell toxicity after the light irradiation, but no toxicity was observed without the light irradiation. Therefore, HP-β-CyD is useful for the preparation of stable C(60) nanoparticles with high ROS generation ability, and C(60)/HP-β-CyD nanoparticles are a promising photosensitizer for photodynamic therapy.

摘要

本研究旨在评估 C(60)/2-羟丙基-β-环糊精(HP-β-CyD)纳米粒子通过光辐照生成活性氧(ROS)和诱导细胞毒性的能力。C(60)纳米粒子是通过在 4°C 下在减压下与 HP-β-CyD 共研磨 3 小时制备的。通过电子自旋共振自旋捕获法和使用 Hela 细胞的细胞活力测试等光谱方法评估了 C(60)/HP-β-CyD 纳米粒子的光动力活性。C(60)/HP-β-CyD 纳米粒子通过光辐照不仅有效地生成了超氧阴离子自由基(O(2)(·-))和羟基自由基(·OH),而且还生成了单线态氧((1)O(2))。通过减小 C(60)纳米粒子的平均粒径,ROS 的生成得到增强,粒径小于 90nm 的粒子显示出高的·OH 和(1)O(2)生成。此外,与聚乙烯吡咯烷酮(C(60)的有效增溶剂)相比,HP-β-CyD 增强了(1)O(2)的生成,这是由于 C(60)部分位于疏水性 CyD 腔中。此外,C(60)/HP-β-CyD 纳米粒子在光照后表现出细胞毒性,但在没有光照的情况下没有观察到毒性。因此,HP-β-CyD 可用于制备具有高 ROS 生成能力的稳定 C(60)纳米粒子,并且 C(60)/HP-β-CyD 纳米粒子是一种有前途的光动力治疗光敏剂。

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