Self-assembly of a 5-fluorouracil and camptothecin dual drug dipeptide conjugate
Self-assembly of a 5-fluorouracil and camptothecin dual drug dipeptide conjugate
复制标题
5-氟尿嘧啶和喜树碱双药二肽缀合物的自组装
DOI：
10.1039/d2ob00762b
复制
发表时间：
2022
影响因子：
3.2
通讯作者：
Parquette, Jon R.
中科院分区：
文献类型：
--
作者：
Sun, Yuan;Fry, Cathleen M.;Shieh, Aileen;Cai, Xiangchen;Reardon, Thomas J.;Parquette, Jon R.
控制药物释放的时空方面的纳米配制的组合疗法具有克服癌症治疗中面临的许多挑战的潜力。在此，我们描述了一种用两种抗癌药物5-氟尿嘧啶（5-FU）和喜树碱（CPT）功能化的肽纳米管。通过肽自组装形成纳米管，其将5-FU定位在水界面的表面上;而CPT被隔离在疏水壁内。因此，观察到两种不同的释放曲线：快速释放5-FU，然后缓慢持续产生CPT。该曲线出现于5-FU在水/纳米管界面处的快速水解裂解，其产生由肽片段组成的较小纳米管。
Nano-formulated, combinatory therapeutics that control the spatiotemporal aspects of drug release have potential to overcome many of the challenges faced in cancer therapy. Herein, we describe a peptide nanotube functionalized with two anticancer drugs, 5-fluoruracil (5-FU) and camptothecin (CPT). The nanotube was formed via peptide self-assembly, which positioned 5-FU on the surface at the aqueous interface; whereas, CPT was sequestered within the hydrophobic walls. Thus, two different release profiles were observed: rapid release of 5-FU, followed by slower, sustained production of CPT. This profile emerged from the rapid hydrolytic cleavage of 5-FU at the aqueous/nanotube interface, which produced a smaller nanotube comprised of the peptide fragment.