醋酸参碱包裹脂质体的经皮传递，显著增强了治疗三阴性乳腺癌的抗肿瘤效果。
Transdermal delivery of brucine-encapsulated liposomes significantly enhances anti-tumor outcomes in treating triple-negative breast cancer.
发表日期：2023 Jul 24
作者：
Min Wu, Yi Hu, Mengran Xu, Lijuan Fu, Chengpan Li, Jingjing Wu, Xin Sun, Wenshen Wang, Shaozhen Wang, Ting Wang, Weiping Ding, Ping Li
来源：
Burns & Trauma
摘要：
三阴性乳腺癌（TNBC）始终是最具挑战性的乳腺癌亚型。在此，我们提出利用多肽修饰脂质体包封的马钱子碱（brucine）通过经皮递送治疗TNBC。我们开发了TD多肽修饰马钱子碱载体脂质体（Bru-TD-Lip），其具有高马钱子碱的包封效率和稳定性。体外实验中，Bru-TD-Lip展示了马钱子碱的经皮渗透能力增强，能够迅速进入TNBC细胞，并显著抑制这些细胞的增殖、迁移和侵袭。体内实验中，通过经皮递送，Bru-TD-Lip具有良好的生物安全性和抗肿瘤活性。Bru-TD-Lip的经皮递送有效靶向并抑制了雌性裸鼠皮下乳腺癌发生。与口服给药相比，经皮递送显著减少了马钱子碱对重要器官的损伤，并增强了马钱子碱治疗TNBC的抗肿瘤效果。本研究为通过马钱子碱治疗三阴性乳腺癌提供了新的治疗策略。版权所有 © 2023. Elsevier B.V.出版
Triple-negative breast cancer (TNBC) is always the most challenging breast cancer subtype. Herein, brucine, encapsulated in peptide-modified liposomes, was proposed for treating TNBC by transdermal delivery. For the TD peptide-modified brucine-loaded liposome (Bru-TD-Lip) we developed, it presents high encapsulation efficiency of brucine and stability. In vitro, Bru-TD-Lip shows the enhanced percutaneous permeability of brucine, is able to readily enter TNBC cells, and significantly inhibits the proliferation, migration, and invasion of these cells. In vivo, through transdermal delivery, Bru-TD-Lip presents good biosafety and anti-tumor efficacy. The transdermal delivery of Bru-TD-Lip effectively targets and inhibits subcutaneous mammary carcinogenesis in female nude mice. Compared with oral administration, the transdermal delivery significantly reduces the damage of brucine to major organs and enhances the antitumor outcomes of brucine in treating TNBC. This study provides a new therapeutic strategy for treating triple-negative breast cancer by brucine.Copyright © 2023. Published by Elsevier B.V.