a Department of Infectious Diseases, The Second Affiliated Hospital of Nanchang University, School of Pharmaceutical Science , Nanchang University , Nanchang PR China.
Drug Deliv. 2019 Dec;26(1):89-97. doi: 10.1080/10717544.2018.1561766.
To prepare sorafenib-loaded folate-decorated bovine serum nanoparticles (FA-SRF-BSANPs) and investigate their effect on the tumor targeting.
The nanoparticles were characterized and evaluated by in vivo and in vitro experiments.
SRF-loaded BSA nanoparticles (SRF-BSANPs) was first prepared and modified with folic acid by chemical coupling to obtain FA-SRF-BSANPs. The average particle size, zeta potential, entrapment efficiency, and drug loading of the optimized FA-SRF-BSANPs were 158.00 nm, -16.27 mV, 77.25%, and 7.73%, respectively. The stability test showed that FA-SRF-BSANPs remained stable for more than 1 month at room temperature. The TEM analysis showed that the surface of FA-SRF-BSANPs was nearly spherical. XRD analysis showed that the drug existed in. the nanoparticles in an amorphous state. FA-SRF-BSANPs can promote the intracellular uptake of hepatoma cells (SMMC-7721) with the strongest inhibitory effect compared with SRF-BSANPs and sorafenib solution. Furthermore, the tumor targeting of FA-SRF-BSANPs (C/C, 0.666 ± 0.053) was significantly higher than those of SRF-BSANPs (C/C, 0.560 ± 0.083) and sorafenib-solution (C/C, 0.410 ± 0.038) in nude mice with liver cancer.
FA-modified albumin nanoparticles are good carriers for delivering SRF to the tumor tissue, which can improve the therapeutic effect and reduce the side effects of the drug.
制备索拉非尼负载叶酸修饰牛血清白蛋白纳米粒(FA-SRF-BSANPs)并考察其对肿瘤的靶向作用。
通过体内和体外实验对纳米粒进行了表征和评价。
首先制备载药牛血清白蛋白纳米粒(SRF-BSANPs),并通过化学偶联法用叶酸进行修饰得到 FA-SRF-BSANPs。优化后的 FA-SRF-BSANPs 的平均粒径、Zeta 电位、包封率和载药量分别为 158.00nm、-16.27mV、77.25%和 7.73%。稳定性试验表明,FA-SRF-BSANPs 在室温下可稳定保存 1 个月以上。TEM 分析表明,FA-SRF-BSANPs 的表面接近球形。XRD 分析表明,药物以无定形状态存在于纳米粒中。与 SRF-BSANPs 和索拉非尼溶液相比,FA-SRF-BSANPs 可促进肝癌细胞(SMMC-7721)的细胞内摄取,抑制作用最强。此外,FA-SRF-BSANPs(C/C,0.666±0.053)的肿瘤靶向性明显高于 SRF-BSANPs(C/C,0.560±0.083)和索拉非尼溶液(C/C,0.410±0.038)在荷肝癌裸鼠体内。
FA 修饰的白蛋白纳米粒是将 SRF 递送到肿瘤组织的良好载体,可提高治疗效果,降低药物的副作用。