Xiao Yanan, Liu Yongjun, Yang Shaomei, Zhang Bo, Wang Tianqi, Jiang Dandan, Zhang Jing, Yu Dexin, Zhang Na
School of Pharmaceutical Science, Shandong University, Jinan, People's Republic of China.
Department of Radiology Medicine, Affiliated Qilu Hospital, Shandong University, Jinan, People's Republic of China.
Colloids Surf B Biointerfaces. 2016 May 1;141:83-92. doi: 10.1016/j.colsurfb.2016.01.016. Epub 2016 Jan 21.
To improve the poor water solubility of sorafenib and to monitor its distribution and the early feedback effects on its in vivo treatment efficacy in a precise manner, sorafenib (SF) and gadolinium (Gd) co-loaded liposomes (SF/Gd-liposomes) were prepared. The simultaneous imaging and therapy efficacies of the SF/Gd-liposomes were tested. The solubility of SF in SF/Gd-liposomes was significantly increased from 0.21 μg/mL to 250 μg/mL. The imaging capability of SF/Gd-liposomes were tested by in-vitro and the in-vivo imaging ability tests and the results confirmed that SF/Gd-liposomes could be served as an effective contrast agent. The design of SF/Gd-liposomes allowed the MRI-guided in vivo visualization of the delivery and biodistribution of liposome. In the in vivo antitumor studies, SF/Gd-liposomes had better antitumor effects in H22 tumor-bearing mice than SF solution (oral or i.v. administration) (P<0.05). These findings indicated that the SF/Gd-liposomes could be used as the promising nano-carriers for the MRI-guided in vivo visualization of the delivery and HCC treatment.
为改善索拉非尼较差的水溶性,并精确监测其分布以及对其体内治疗效果的早期反馈作用,制备了索拉非尼(SF)和钆(Gd)共载脂质体(SF/Gd-脂质体)。测试了SF/Gd-脂质体的同步成像和治疗效果。SF在SF/Gd-脂质体中的溶解度从0.21μg/mL显著提高至250μg/mL。通过体外和体内成像能力测试对SF/Gd-脂质体的成像能力进行了测试,结果证实SF/Gd-脂质体可作为一种有效的造影剂。SF/Gd-脂质体的设计使得脂质体的递送和生物分布能够在MRI引导下于体内可视化。在体内抗肿瘤研究中,SF/Gd-脂质体在荷H22肿瘤小鼠中比索拉非尼溶液(口服或静脉给药)具有更好的抗肿瘤效果(P<0.05)。这些研究结果表明,SF/Gd-脂质体可作为有前景的纳米载体,用于MRI引导下脂质体递送的体内可视化及肝癌治疗。