Highly Fluorinated Graphene Oxide Nanosheets for Anticancer Linoleic-Curcumin Conjugate Delivery and T2-Weighted Magnetic Resonance Imaging: In Vitro and in Vivo Studies Publisher



Razaghi M¹ ; Ramazani A¹ ; Khoobi M^{2, 3} ; Mortezazadeh T⁴ ; Aksoy EA⁵ ; Kucukkilinc TT⁶ Show Affiliations
Source: Journal of Drug Delivery Science and Technology Published:2020

Abstract

Carbon-based nanomaterials have received substantial attention as a drug delivery platform for cancer treatment. In the current study, a simple and eco-friendly method was introduced for the preparation of highly fluorinated graphene oxide (FGO), which was subsequently evaluated by standard characterization methods. It was then employed as a carrier for Linoleic acid-curcumin conjugate as an anticancer drug (FGO-Lino-CUR). Finally, the release profile and selective toxicity of FGO-Lino-CUR were investigated and compared with FGO-CUR. It was observed that the pH-sensitive release fitted to Korsmeyer–Peppas model. The accumulated release of Lino-CUR at pH 5.5 was about 20% more than that of pH 7.4. FGO-Lino-CUR exhibited relatively high toxicity (about 60%) against MCF-7 cells which was 20% more than that against MCF10A cells. In vitro MRI studies also revealed that the Lino-CUR loaded FGO with adequate relaxation rate (r2 = 67.12 (s−1mM−1)) and favorable ability to reduce signal intensity in the presence of MCF10A and MCF-7 cells, could be a potential candidate as a negative MRI contrast agent. In vivo anti-tumor studies were performed on 4T1 induced BALB/c breast cancer model. Accordingly, the higher tumor suppression capability of FGO-Lino-CUR was observed with no significant body weight changes during treatment compared with free Lino-CUR. Moreover, the MRI contrast enhancing ability of FGO-Lino-CUR for the in vivo MRI of tumor bearing BALB/c mice, indicated its noticeable ability to create negative contrast. Simple and versatile method for the preparation of the target system as well as acceptable anticancer activity and MRI contrast enhancement, make Lino-CUR loaded FGO as an encouraging candidate for the breast cancer theranostics. © 2020 Elsevier B.V.