Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, G4 0RE, UK.
College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, G12 8QQ, UK.
Int J Nanomedicine. 2021 Apr 6;16:2615-2631. doi: 10.2147/IJN.S293480. eCollection 2021.
Plumbagin, a naphthoquinone extracted from the officinal leadwort presenting promising anti-cancer properties, has its therapeutic potential limited by its inability to reach tumors in a specific way at a therapeutic concentration following systemic injection. The purpose of this study is to assess whether a novel tumor-targeted, lipid-polymer hybrid nanoparticle formulation of plumbagin would suppress the growth of B16-F10 melanoma in vitro and in vivo.
Novel lipid-polymer hybrid nanoparticles entrapping plumbagin and conjugated with transferrin, whose receptors are present in abundance on many cancer cells, have been developed. Their cellular uptake, anti-proliferative and apoptosis efficacy were assessed on various cancer cell lines in vitro. Their therapeutic efficacy was evaluated in vivo after tail vein injection to mice bearing B16-F10 melanoma tumors.
The transferrin-bearing lipid-polymer hybrid nanoparticles loaded with plumbagin resulted in the disappearance of 40% of B16-F10 tumors and regression of 10% of the tumors following intravenous administration. They were well tolerated by the mice.
These therapeutic effects, therefore, make transferrin-bearing lipid-polymer hybrid nanoparticles entrapping plumbagin a highly promising anti-cancer nanomedicine.
从药用白头翁中提取的萘醌类化合物白花丹素具有有前景的抗癌特性，但由于其在全身注射后不能以治疗浓度以特定方式到达肿瘤，因此其治疗潜力受到限制。本研究旨在评估新型肿瘤靶向脂质-聚合物杂化纳米颗粒制剂白花丹素是否能抑制体外和体内 B16-F10 黑色素瘤的生长。
已经开发了新型的脂质-聚合物杂化纳米颗粒，其包封白花丹素并与转铁蛋白缀合，转铁蛋白受体在许多癌细胞中大量存在。在体外评估了它们在各种癌细胞系中的细胞摄取、抗增殖和凋亡功效。在尾静脉注射携带 B16-F10 黑色素瘤肿瘤的小鼠后，评估了它们的治疗功效。
负载白花丹素的带转铁蛋白的脂质-聚合物杂化纳米颗粒导致 40%的 B16-F10 肿瘤消失，并且静脉给药后 10%的肿瘤消退。它们被小鼠很好地耐受。
因此，这些治疗效果使得负载白花丹素的带转铁蛋白的脂质-聚合物杂化纳米颗粒成为一种很有前途的抗癌纳米药物。
Zotero 插件
