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载索拉非尼的叶酸修饰牛血清白蛋白纳米粒增强对肝肿瘤的药物靶向作用。

Improved drug targeting to liver tumor by sorafenib-loaded folate-decorated bovine serum albumin nanoparticles.

机构信息

a Department of Infectious Diseases, The Second Affiliated Hospital of Nanchang University, School of Pharmaceutical Science , Nanchang University , Nanchang PR China.

出版信息

Drug Deliv. 2019 Dec;26(1):89-97. doi: 10.1080/10717544.2018.1561766.

Abstract

BACKGROUND

To prepare sorafenib-loaded folate-decorated bovine serum nanoparticles (FA-SRF-BSANPs) and investigate their effect on the tumor targeting.

METHODS

The nanoparticles were characterized and evaluated by in vivo and in vitro experiments.

RESULTS

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.

CONCLUSION

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.

摘要

背景

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。

方法

通过体内和体外实验对纳米粒进行了表征和评价。

结果

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。

结论

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f81a/6374969/49c13180f72c/IDRD_A_1561766_F0001_C.jpg

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