Department of Biological Sciences, Sunandan Divatia School of Science, SVKM's NMIMS (Deemed-to-be University), Vile Parle (West), Mumbai 400056, India.
Nanoscale. 2018 May 3;10(17):8031-8041. doi: 10.1039/c7nr09503a.
The anticancer properties of arsenic trioxide (As2O3) are accompanied by highly cytotoxic effects on normal cells. This necessitates developing modalities towards the targeted delivery of As2O3. Albumins, on account of their large structure and presence of several interacting groups, are ideal for encapsulating or carrying various drugs. In the present study, human serum albumin (HSA) was chosen as a coating agent to increase the biocompatibility of As2O3. An in situ chemical precipitation method was adopted for the synthesis of HSA-coated As2O3 nanoparticles (HSA-As2O3NPs) that were further characterized by Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), ultraviolet-visible (UV-vis) spectroscopy, inductively coupled plasma atomic emission spectrometry (ICP-AES), zeta potential and transmission electron microscopy (TEM). HSA-As2O3NPs were assessed for their biocompatibility using mouse fibroblast cells (NIH-3T3) and human dermal fibroblast (HDF) cells by a time- and dose-dependent cytocompatibility MTT assay. The safety of the HSA-As2O3 nanoparticles was assessed using haemolysis and blood cell aggregation studies. Molecular simulation studies provided evidence of interaction between HSA and As2O3. Herein, we report the development of a protein-based delivery system for As2O3 with improved biocompatibility.
三氧化二砷（As2O3）具有抗癌特性，但对正常细胞具有很强的细胞毒性。这就需要开发针对 As2O3 的靶向递药方式。白蛋白由于其较大的结构和存在多个相互作用的基团，是包裹或携带各种药物的理想选择。在本研究中，选择人血清白蛋白（HSA）作为涂层剂来提高 As2O3 的生物相容性。采用原位化学沉淀法合成了 HSA 包覆的 As2O3 纳米颗粒（HSA-As2O3NPs），并通过傅里叶变换红外光谱（FT-IR）、X 射线衍射（XRD）、紫外-可见（UV-vis）光谱、电感耦合等离子体原子发射光谱（ICP-AES）、zeta 电位和透射电子显微镜（TEM）对其进行了表征。通过时间和剂量依赖性细胞相容性 MTT 测定法，使用小鼠成纤维细胞（NIH-3T3）和人皮肤成纤维细胞（HDF）评估 HSA-As2O3NPs 的生物相容性。通过溶血和血细胞聚集研究评估了 HSA-As2O3 纳米颗粒的安全性。分子模拟研究提供了 HSA 与 As2O3 之间相互作用的证据。在此，我们报告了一种基于蛋白质的 As2O3 递药系统的开发，该系统具有改善的生物相容性。
