Alhourani Abdelnour, Førde Jan-Lukas, Eichacker Lutz Andreas, Herfindal Lars, Hagland Hanne Røland
Department of Chemistry, Biosciences and Environmental Technology, University of Stavanger, 4021 Stavanger, Norway.
Centre for Pharmacy, Department of Clinical Science, University of Bergen, 5007 Bergen, Norway.
ACS Omega. 2021 Sep 14;6(38):24619-24629. doi: 10.1021/acsomega.1c03283. eCollection 2021 Sep 28.
Graphene-based drug carriers provide a promising addition to current cancer drug delivery options. Increased accessibility of high-quality graphene made by plasma-enhanced chemical vapor deposition (PE-CVD) makes it an attractive material to revisit in comparison to the widely studied graphene oxide (GO) in drug delivery. Here, we show the potential of repurposing the metabolic drug phenformin for cancer treatment in terms of stability, binding, and pH-responsive release. Using covalent attachment of poly(ethylene glycol) (PEG) onto pristine (PE-CVD) graphene, we show that PEG stabilized graphene nanosheets (PGNS) are stable in aqueous solutions and exhibit higher binding affinity toward phenformin than GO. Moreover, we experimentally demonstrate an improved drug release from PGNS than GO at pH levels lower than physiological conditions, yet comparable to that found in tumor microenvironments.
基于石墨烯的药物载体为当前癌症药物递送选择增添了一个有前景的补充。与在药物递送中被广泛研究的氧化石墨烯（GO）相比，通过等离子体增强化学气相沉积（PE-CVD）制备的高质量石墨烯的可及性增加，使其成为一种值得重新审视的有吸引力的材料。在此，我们展示了将代谢药物二甲双胍重新用于癌症治疗在稳定性、结合和pH响应释放方面的潜力。通过将聚乙二醇（PEG）共价连接到原始（PE-CVD）石墨烯上，我们表明PEG稳定的石墨烯纳米片（PGNS）在水溶液中稳定，并且对二甲双胍的结合亲和力高于GO。此外，我们通过实验证明，在低于生理条件的pH水平下，PGNS的药物释放比GO有所改善，但与肿瘤微环境中的情况相当。
