Master's Degree Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.
Laboratory of Physical Chemistry, Molecular and Cellular Biology, Department of Radiologic Technology, Faculty of Associated Medical Sciences, Chiang Mai University, Chiang Mai, Thailand.
J Pharm Sci. 2019 Feb;108(2):996-1006. doi: 10.1016/j.xphs.2018.08.008. Epub 2018 Aug 16.
The aim of this study is to develop co-encapsulation of quercetin (QCT) and superparamagnetic iron oxide nanoparticles (SPIONs) into methoxy-poly(ethylene glycol)-b-oligo(ɛ-caprolactone), mPEG750-b-OCL-Bz micelles (QCT-SPION-loaded micelles) for inhibition of hepatitis B virus-transfected hepatocellular carcinoma (HepG2.2.15) cell growth. QCT-SPION-loaded micelles were prepared using film hydration method. They were spherical in shape with an average size of 22-55 nm. The best QCT-SPION-loaded micelles showed entrapment efficiency and loading capacity of QCT at 70% and 3.5%, respectively, and of SPIONs at 15% and 0.8%, respectively. Transverse (T) relaxivity of SPIONs was 137 mMs. SPION clusters present inside the core of QCT-SPION-loaded micelles increased T relaxivity value (246 mMs) indicating the good magnetic resonance imaging sensitivity of QCT-SPION-loaded micelles in comparison with SPIONs. QCT-SPION-loaded micelles could be taken up by HepG2.2.15 cells and showed higher cytotoxicity than QCT. Furthermore, these cells were arrested by QCT-SPION-loaded micelles at the G0/G1 phase of cell cycle. QCT-SPION-loaded micelles accumulated in the vicinity of Neodymium Iron Boron (NdFeB) magnetic disc, resulting in the potent inhibition of cancer cell growth at the strong magnetic field strength. In conclusion, mPEG750-b-OCL-Bz micelles are a promising multi-functional vehicle for co-delivery of QCT and SPIONs for disease monitoring and therapies of hepatocellular carcinoma.
本研究旨在开发将槲皮素(QCT)和超顺磁性氧化铁纳米粒子(SPIONs)共包封到甲氧基聚乙二醇-b-聚(ε-己内酯),mPEG750-b-OCL-Bz 胶束(QCT-SPION 负载胶束)中,以抑制乙型肝炎病毒转染的肝癌(HepG2.2.15)细胞生长。QCT-SPION 负载胶束采用薄膜水化法制备。它们呈球形,平均粒径为 22-55nm。最佳的 QCT-SPION 负载胶束的 QCT 包封效率和载药量分别为 70%和 3.5%,SPIONs 的包封效率和载药量分别为 15%和 0.8%。SPIONs 的横向(T)弛豫率为 137mMs。存在于 QCT-SPION 负载胶束核心内的 SPION 簇增加了 T 弛豫率值(246mMs),表明与 SPIONs 相比,QCT-SPION 负载胶束具有良好的磁共振成像灵敏度。QCT-SPION 负载胶束可被 HepG2.2.15 细胞摄取,并表现出比 QCT 更高的细胞毒性。此外,这些细胞被 QCT-SPION 负载胶束阻滞在细胞周期的 G0/G1 期。QCT-SPION 负载胶束在钕铁硼(NdFeB)磁盘附近积聚,导致在强磁场强度下有效地抑制癌细胞生长。总之,mPEG750-b-OCL-Bz 胶束是一种有前途的多功能载体,可用于共递送 QCT 和 SPIONs,用于肝癌的疾病监测和治疗。
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