Nanobiotechnology Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran; Faculty of Pharmacy, Baqiyatallah University of Medical Sciences, Tehran, Iran.
Department of Pharmaceutical Biomaterials, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
Bioorg Chem. 2020 Jul;100:103891. doi: 10.1016/j.bioorg.2020.103891. Epub 2020 May 7.
In this research, curcumin (CUR) conjugated albumin based nanoparticles (BSA-CUR) were designed for improvement and evaluation radioprotective effect of CUR. In this way, we have prepared BSA-CUR by covalently binding the CUR with BSA. Next, this synthesized prodrug was evaluated for physical and chemical properties by Fourier-transform infrared (FTIR), Dynamic light scattering (DLS), Transmission electron microscopy (TEM), Ultraviolet-visible (UV/Vis), and Differential scanning calorimetry (DSC) analysis. Furthermore, the chemical stability of designed prodrug was appraised. The result shows that the size of nanoparticles is 174.4 nm with a polydispersity index (PdI) of 0.191. The nanoparticles have a high loading capacity and show sustained release behavior. Loading of CUR to BSA not only could increase the chemical stability of CUR, but also could improve radioprotection efficacy of it's against X-Ray irradiation. The HHF-2 cells show 107% viability in the presence of BSA-CUR at a concentration of 50 µg/mL, whereas non-treated cells show 46% viability, under X-Ray irradiation. Also in vivo study results show that, four out of five mice have died when the mice irradiated by X-Ray and no received any treatment. Although, for a group that treated with BSA-CUR and also irradiated by X-Ray, median survival and survival rate was higher than CUR treated and control mice, and only two out of five mice have died. The result of this study proved that BSA-CUR can be used as a proficient vehicle for improving the potential radioprotective effect of CUR.
在这项研究中,设计了姜黄素(CUR)结合白蛋白的纳米粒子(BSA-CUR),以提高和评估 CUR 的放射防护作用。通过这种方式,我们通过将 CUR 与 BSA 共价结合来制备 BSA-CUR。接下来,通过傅里叶变换红外(FTIR)、动态光散射(DLS)、透射电子显微镜(TEM)、紫外-可见(UV/Vis)和差示扫描量热法(DSC)分析来评估该合成前药的物理和化学性质。此外,还评估了设计的前药的化学稳定性。结果表明,纳米粒子的粒径为 174.4nm,多分散指数(PdI)为 0.191。纳米粒子具有高载药量并表现出持续释放行为。CUR 加载到 BSA 不仅可以增加 CUR 的化学稳定性,还可以提高其对 X 射线照射的放射防护效果。在浓度为 50μg/mL 时,BSA-CUR 存在的情况下,HHF-2 细胞的活力为 107%,而未经处理的细胞的活力为 46%,在 X 射线照射下。体内研究结果还表明,在 X 射线照射且未接受任何治疗的情况下,五分之四的小鼠死亡。然而,对于用 BSA-CUR 治疗并用 X 射线照射的一组,中位存活时间和存活率高于 CUR 治疗和对照组的小鼠,只有五分之二的小鼠死亡。这项研究的结果证明,BSA-CUR 可以用作提高 CUR 潜在放射防护作用的有效载体。