天然Coptidis树瘤纳米颗粒改善了Docetaxel的口服输送
Dan Ye1, Ding Ding1, Ling-Yun Pan2
1Department of Pharmacology, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People's Republic of China.
International journal of nanomedicine
|August 23, 2024
概括
自然纳米颗粒 (Nnps) 有效地通过口服输送多塞 (DTX). 该系统增强了DTX的溶解性,吸收和抗瘤活性,提供了一种有前途的新化疗方法.
科学领域:
- 纳米技术纳米技术
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
背景情况:
- 多塞塔克塞尔 (DTX) 是一种关键的抗瘤药物,口服生物可用性差.
- 开发有效的DTX口服输送系统对于改善患者遵守和治疗结果至关重要.
研究的目的:
- 开发使用天然纳米粒子 (Nnps) 的多塞 (DTX) 口服药物输送系统.
- 描述DTX载荷Nnps (Nnps-DTX) 的物理化学特性,体外性能和体内药理动力学.
- 为了评估Nnps-DTX的抗瘤疗效.
主要方法:
- 用DTX装载的自组装纳米粒子 (Nnps-DTX) 用热感应方法制备.
- 描述包括尺寸,Zeta潜力,封装效率,负载能力和稳定性.
- 在体外研究中评估了溶解性,释放动力学,细胞吸收和代谢稳定性.
- 在体内评估了针对瘤细胞系的药理动力学和细胞毒性.
主要成果:
- Nnps-DTX表现出最佳的特性:球形,138.6 nm大小,-20.8 mV Zeta潜力,77.6%的封装效率和6.8%的负载能力.
- 与自由DTX相比,Nnps-DTX显示溶解度增加了23.3倍,并增强了药物释放.
- 口服Nnps-DTX显著增加了血液和器官中的DTX度,通过洞穴介导的内分泌细胞增强细胞吸收.
- Nnps-DTX表现出改善的代谢稳定性和强大的细胞毒性对抗MCF-7,HCT116和HepG2细胞.
结论:
- 开发的Nnps-DTX系统显著改善了口服多塞的生物可用性,溶解性和释放性.
- Nnps-DTX表现出增强的细胞吸收,代谢稳定性和强大的抗瘤活性.
- 这种新型纳米粒子配方代表了在癌症治疗中口服多塞塔克塞尔输送的有希望的策略.
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