开发和表征优化药物载荷的体,用于输送5-FU和伊利诺德坎
Kafilat O Agbaje1, Simeon K Adesina1, Amusa S Adebayo1
1Department of Pharmaceutical Sciences, College of Pharmacy, Howard University, 2300 4th Street NW, Washington, DC 20059, USA.
Pharmaceutics
|July 30, 2025
概括
这项研究开发了纳米封装的5-Fluorouracil (5-FU) 和Irinotcan (IRT) 在体和结肠特异性囊中,以改善结肠直肠癌 (CRC) 治疗治疗和降低毒性.
科学领域:
- 纳米技术 纳米技术
- 制药科学 制药科学
- 在瘤学瘤学.
背景情况:
- 结肠直肠癌 (CRC) 治疗面临的挑战是5-Fluorouracil (5-FU) 和Irinotcan (IRT) 由于药物输送不良和全身毒性.
- 5-FU和IRT的组合显示出协同作用,但受到短半衰期和非目标效应的限制.
- 需要新的药物输送系统来提高治疗疗效,并尽量减少CRC治疗中的副作用.
研究的目的:
- 开发一种纳米封装策略,用于在体中同时提供5-FU和IRT.
- 通过在结肠特异性囊中过度封装冷化体来增强CRC向和减少系统分布.
- 评估纳米配方的物理化学特性和体外药物释放.
主要方法:
- 用薄膜水化方法制备封装5-FU和IRT的体.
- 使用实验设计 (DOE) 软件优化了配方变量.
- 体的特征包括大小,多分散性指数 (PDI),形态和药物负载.
- 实验室药物释放研究是在生物相关介质中进行的.
主要成果:
- 同封装的体平均为251nm,PDI为0.293,表明良好的均性.
- 表面活性剂与胆固醇的比率显著影响了阴酶体大小和PDI.
- 水友性5-FU显示出比脂友性IRT更高的负载效率.
- 在体外研究表明,IRT和5-FU分别在下肠和结肠区域的释放延迟.
结论:
- 在体中对5-FU/IRT进行同纳米封装,然后在结肠特异性囊中进行冷化和封装,为CRC治疗提供了一种有前途的方法.
- 这一策略促进了CRC微环境的被动向,有可能改善药物输送和减少系统毒性.
- 开发的配方显示了在治疗结直肠癌方面提高疗效的潜力.
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