基于酸盐的智能胃阻塞药物输送系统,用于用revaprazan装载的SLN;配方和表征
Hadiqa Nazish Raja1, Fakhar Ud Din1, Kanwal Shabbir1
1Nanomedicine Research Group, Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan; Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan.
International journal of biological macromolecules
|October 13, 2023
概括
装入胃系统固体脂质纳米颗粒 (GRS/REV-SLNs) 的revaprazan (REV) 改善了药物的溶解和生物可用性. 这种新的系统增强了胃的保留,为胃提供了一个有前途的新治疗方法.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 一种质子抑制剂 (PPI) Revaprazan (REV) 溶解不良,半衰期短,限制了其治疗胃潰瘍的有效性.
- 固体脂质纳米颗粒 (SLN) 被认为具有提高脂性药物的溶解和生物可用性的潜力.
研究的目的:
- 开发和优化REV装载SLN (GRS/REV-SLN) 的胃保持系统.
- 为了提高Revaprazan的生物可用性和胃留.
主要方法:
- 用REV装载的SLN的配方和特征,包括颗粒大小,PDI,zeta潜力和药物整合效率.
- 在小鼠中使用体外凝,浮力研究和体内药理动力学评估来评估GRS/REV-SLNs.
- 通过传输电子显微镜 (TEM) 进行形态分析和使用福里埃变换红外光谱 (FTIR) 进行化学相互作用分析.
主要成果:
- 优化REV-SLN的颗粒大小为120nm,PDI为0.313,zeta潜力为-20.7mV,药物整合率为88%.
- 实验室研究表明,GRS/REV-SLN的持续凝和浮力持续超过12小时.
- 在老鼠体内实验证实了成功的胃转化,并改善了Revaprazan的生物可用性.
结论:
- 开发的GRS/REV-SLNs系统有效地提高了Revaprazan的胃保留和生物可用性.
- 这种新型药物输送系统为治疗胃潰瘍提供了一种潜在的改善治疗方法.
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