微针贴片提供PROTACs用于抗癌疗法
Xiao Cheng1,2, Shiqi Hu1,2, Ke Cheng1,2
1Joint Department of Biomedical Engineering, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States, and North Carolina State University, Raleigh, North Carolina 27606, United States.
ACS nano
|June 9, 2023
概括
微针贴片使得瘤能够直接输送向蛋白质分解的仿真体 (PROTACs),从而提高药物溶解性和向,从而改善癌症治疗. 这种方法显示显著的瘤减少和良好的安全性.
科学领域:
- 生物技术是生物技术.
- 在瘤学瘤学.
- 药物输送系统 药物输送系统
背景情况:
- 向蛋白质分解的仿真体 (PROTACs) 为治疗疾病提供了一种新的蛋白质降解方法.
- 目前PROTAC的局限性包括溶解性差和缺少器官向性,阻碍了临床应用.
- 有效地将PROTACs传递到向组织仍然是一个重大挑战.
研究的目的:
- 开发和评估微针贴片,以直接和持续地向瘤输送PROTACs.
- 为了评估微针传递的ERα降解PROTAC (ERD308) 与ER阳性乳腺癌的Palbociclib结合的治疗疗效.
主要方法:
- 封装ERD308和Palbociclib在pH敏感的MPEG-PAE微粒中.
- 装载药物装载的小球体进入可生物降解的微针贴片,用于通过皮肤输送.
- 在MCF7细胞中对ERα降解的体外评估和瘤减少和安全的体内评估.
主要成果:
- 微针贴片在瘤中实现了长时间的药物释放 (≥4天) 和高药物保留率 (>87%).
- 从补丁中释放的ERD308有效降解了癌细胞中的ERα.
- 组合疗法证明了超过80%的瘤减少,具有有利的安全性.
结论:
- 微针贴片为直接和持续向瘤输送PROTACs提供了一个可行的平台.
- 这种输送系统克服了PROTAC的局限性,显示了ER阳性乳腺癌的治疗潜力.
- 该研究验证了在瘤学中基于微针的PROTAC输送的概念验证.
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