载喜树碱前药和姜黄素的脂质体肺部递药用于肺癌治疗。
Pulmonary delivery of liposomes co-loaded with SN38 prodrug and curcumin for the treatment of lung cancer.
机构信息
School of Pharmacy and Bioengineering, Chongqing University of Technology, 69 Hongguang Road, Chongqing 400054, China.
Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, Innovative Drug Research Center, School of Pharmaceutical Sciences, Chongqing University, 55 South Daxuecheng Road, Chongqing 401331, China.
出版信息
Eur J Pharm Biopharm. 2022 Oct;179:156-165. doi: 10.1016/j.ejpb.2022.08.021. Epub 2022 Sep 5.
A co-delivery system of SN38 (7-ethyl-10-hydroxyl camptothecin) prodrug and CUR (curcumin) was designed for the treatment of lung cancer by pulmonary delivery. SN38 was linked to cell-penetrating peptide (CPP) TAT via a polyethylene glycol (PEG) linker to form the SN38 prodrug (TAT-PEG-SN38). Liposomes co-loaded with amphiphilic TAT-PEG-SN38 and curcumin (Lip-TAT-PEG-SN38/CUR) were successfully prepared by a microfluidic method for the treatment of lung cancer via pulmonary delivery. Lip-TAT-PEG-SN38/CUR showed nanometer-sized sphericity and a particle size of 171.21 nm. Besides, Lip-TAT-PEG-SN38/CUR exhibited enhanced antiproliferative effect, increased cell apoptosis induction and improved cell cycle arrest compared to the single agents in vitro. The combination induced significant tumor inhibition in a BALB/c mouse lung cancer model. These results indicated that our SN38 prodrug and curcumin co-delivery system was a promising candidate for lung cancer treatment.
通过肺部给药，设计了一种 SN38（7-乙基-10-羟基喜树碱）前药和 CUR（姜黄素）的共递送系统，用于治疗肺癌。SN38 通过聚乙二醇（PEG）接头与穿膜肽（CPP）TAT 相连，形成 SN38 前药（TAT-PEG-SN38）。通过微流控法成功制备了载有两亲性 TAT-PEG-SN38 和姜黄素的脂质体（Lip-TAT-PEG-SN38/CUR），用于通过肺部给药治疗肺癌。Lip-TAT-PEG-SN38/CUR 呈纳米级球形，粒径为 171.21nm。此外，Lip-TAT-PEG-SN38/CUR 在体外表现出比单一药物更强的抗增殖作用、增加细胞凋亡诱导和改善细胞周期停滞的作用。该组合在 BALB/c 小鼠肺癌模型中诱导了显著的肿瘤抑制作用。这些结果表明，我们的 SN38 前药和姜黄素共递送系统是治疗肺癌的有前途的候选药物。
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