Fujian Provincial Key Laboratory of Innovative Drug Target Research, School of Pharmaceutical Sciences, Xiamen University, Xiamen, China.
State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics and Center for Molecular Imaging and Translational Medicine, School of Public Health, Xiamen University, Xiamen, China.
J Control Release. 2018 Feb 28;272:145-158. doi: 10.1016/j.jconrel.2017.04.028. Epub 2017 Apr 23.
Precise delivery of antineoplastic drugs to specific tumor region has drawn much attention in recent years. Herein, a light/magnetic hyperthermia triggered drug delivery with multiple functionality is designed based on methotrexate (MTX) modified thermo-sensitive magnetoliposomes (MTX-MagTSLs). In this system, MTX and oleic acid modified magnetic nanoparticles (MNPs) can be applied in biological and magnetic targeting. Meanwhile, lipophilic fluorescent dye Cy5.5 and MNPs are encapsulated into the bilayer of liposomes, which can not only achieve dual-imaging effect to verify the MTX-MagTSLs accumulation in tumor region, but also provide an appropriate laser irradiation region to release Doxorubicin (Dox) under alternating magnetic field (AMF). Both in vitro and in vivo results revealed that MTX-MagTSLs possessed an excellent targeting ability towards HeLa cells and HeLa tumor-bearing mice. Furthermore, the heating effect of MTX-MagTSLs was amplified 4.2-fold upon combination with AMF and local precise near-infrared laser irradiation (808nm) (DUAL-mode) to rapidly reach the phase change temperature (Tm) of MTX-MagTSLs in 5min compared with either AMF or laser stimulation alone, resulting in a significantly enhanced release of Dox at tumor region and precise cancer synergetic theranostics.
近年来,将抗肿瘤药物精确递送到特定肿瘤区域引起了广泛关注。在此,基于甲氨蝶呤(MTX)修饰的热敏磁脂质体(MTX-MagTSLs)设计了一种具有多重功能的光/磁热疗触发药物递送系统。在该系统中,MTX 和油酸修饰的磁性纳米颗粒(MNPs)可用于生物和磁靶向。同时,亲脂性荧光染料 Cy5.5 和 MNPs 被包裹在脂质体的双层中,不仅可以实现双重成像效果以验证 MTX-MagTSLs 在肿瘤区域的积累,还可以提供适当的激光照射区域,以便在交变磁场(AMF)下释放阿霉素(Dox)。体外和体内结果均表明,MTX-MagTSLs 对 HeLa 细胞和 HeLa 荷瘤小鼠具有优异的靶向能力。此外,MTX-MagTSLs 在与 AMF 和局部精确近红外激光照射(808nm)(DUAL 模式)结合后,其加热效果放大了 4.2 倍,与单独使用 AMF 或激光刺激相比,在 5min 内迅速达到 MTX-MagTSLs 的相变温度(Tm),从而在肿瘤区域显著增强了 Dox 的释放,并实现了精确的癌症协同治疗。
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