自体乳化药物输送系统:干湿逆微粒的比较
Numan Eczacioglu1, Annika Postina2, Melanie Ebert2
1Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, Innsbruck 6020, Austria; Department of Bioengineering, Karamanoğlu Mehmetbey University, 70110 Karaman, Türkiye.
Acta biomaterialia
|July 14, 2025
概括
干逆 (dRMs) 在自我乳化药物递送系统 (SEDDS) 中表现优于湿逆 (wRMs). 在SEDDS配方中,dRMs提供了增强的封装,改善了模型蛋白质的口服生物可用性,以及更好的安全性.
科学领域:
- 纳米技术 纳米技术
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 在提高口服生物可用性和基药物的稳定性方面,仍然存在挑战.
- 反向微粒 (RMs) 是药物输送的有希望的纳米载体,提供高封装效率和防腐保护.
- 在自乳化药物输送系统 (SEDDS) 中,需要对干逆菌体 (dRMs) 和湿逆菌体 (wRMs) 进行比较评估.
研究的目的:
- 为了比较dRMs和wRMs在SEDDS中的药物输送性能.
- 评估关键参数,包括逆临界细胞度 (rCMC),捕获效率 (EE) 和分区系数 (logD).
- 评估药物载体SEDDS-RMs的细胞毒性,细胞吸收,膜透性和体内口服生物利用性.
主要方法:
- 使用各种表面活性剂形成RM,并加入模型染料.
- RMs和SEDDS-RMs的表征,包括rCMC,EE,logD,尺寸分布,PDI和泽塔潜力.
- 在体外细胞毒性,Caco-2细胞膜透性研究,以及在小鼠体内药物动力学研究,使用大过氧化酶 (HRP) 作为模型药物.
主要成果:
- 与wRMs (logD 0.59,EE 74%) 相比,基于比单酸盐的dRMs显示出更高的logD (1.56) 和EE (97%).
- 与SEDDS-wRMs (13.5倍) 相比,SEDDS-dRMs的细胞毒性显著降低,膜透性提高 (7.5倍).
- 在老鼠中,口服HRP加载的SEDDS-dRMs导致生物可用性更高 (11.2%) 比SEDDS-wRMs (7.9%).
结论:
- 在SEDDS配方中,干逆 (dRMs) 显示出优于湿逆 (wRMs) 的性能.
- 在药物加载,稳定性,细胞透性和口服生物利用性方面,dRM具有优势,使其成为SEDDS的首选选择.
- 这些发现支持基于dRM的SEDDS作为一种有效的纳米载体系统的潜力,用于口服提供具有挑战性的治疗方法,包括蛋白质和类药物.
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