Diaz-Galvez Kevin R, Teran-Saavedra Nayelli G, Burgara-Estrella Alexel J, Fernandez-Quiroz Daniel, Silva-Campa Erika, Acosta-Elias Monica, Sarabia-Sainz Hector M, Pedroza-Montero Martín R, Sarabia-Sainz Jose A
Departamento de Investigación en Polímeros y Materiales, Universidad de Sonora Hermosillo Mexico.
Departamento de Investigación en Física, Universidad de Sonora Hermosillo Mexico
RSC Adv. 2019 Mar 29;9(18):9899-9906. doi: 10.1039/c8ra09732a. eCollection 2019 Mar 28.
In this work, we report the evaluation of lactosylated graphene oxide (GO-AL) as a potential drug carrier targeted at an asialoglycoprotein receptor (ASGPR) from hepatic cancer cells. Structural-modification, safety evaluation, and functional analysis of GO-AL were performed. The structure and morphology of the composite were analyzed by scanning electron microscopy (SEM) and atomic force microscopy (AFM), while Raman and FTIR spectroscopy were used to track the chemical modification. For the safe application of GO-AL, an evaluation of the cytotoxic effect, hemolytic properties, and specific interactions of the glycoconjugate were also studied. SEM and AFM analysis of the GO showed graphene sheets with a layer size of 2-3 nm, though a few of them reached 4 nm. The Raman spectra presented characteristic peaks of graphene oxide at 1608 cm and 1350 cm, corresponding to G and D bands, respectively. Besides, Si-O peaks for the APTES conjugates of GO were identified by FTIR spectroscopy. No cytotoxic or hemolytic effects were observed for GO samples, thus proving their biocompatibility. The interaction of lectin confirmed that GO-AL has a biorecognition capability and an exposed galactose structure. This biorecognition capability was accompanied by the determination of the specific absorption of lactosylated GO by HepG2 cells mediated through the asialoglycoprotein receptor. The successful conjugation, hemolytic safety, and specific recognition described here for lactosylated GO indicate its promise as an efficient drug-delivery vehicle to hepatic tissue.
在本研究中，我们报告了对乳糖基化氧化石墨烯（GO-AL）作为一种靶向肝癌细胞去唾液酸糖蛋白受体（ASGPR）的潜在药物载体的评估。对GO-AL进行了结构修饰、安全性评估和功能分析。通过扫描电子显微镜（SEM）和原子力显微镜（AFM）分析了复合材料的结构和形态，同时利用拉曼光谱和傅里叶变换红外光谱（FTIR）追踪化学修饰。为了GO-AL的安全应用，还研究了其细胞毒性作用、溶血特性以及糖缀合物的特异性相互作用。对GO的SEM和AFM分析显示石墨烯片层尺寸为2 - 3 nm，不过其中少数达到4 nm。拉曼光谱在1608 cm和1350 cm处呈现氧化石墨烯的特征峰，分别对应G带和D带。此外，通过FTIR光谱鉴定了GO的APTES缀合物的Si - O峰。未观察到GO样品的细胞毒性或溶血作用，从而证明了它们的生物相容性。凝集素的相互作用证实GO-AL具有生物识别能力和暴露的半乳糖结构。这种生物识别能力伴随着通过去唾液酸糖蛋白受体介导的HepG2细胞对乳糖基化GO的特异性吸收的测定。此处描述的乳糖基化GO的成功缀合、溶血安全性和特异性识别表明其有望成为一种高效的肝组织药物递送载体。
