在动物模型中,用天然化合物鲁布索西德溶解帕克利塔克塞尔,以改善口服生物可用性
Jian Zhang1,2, Jicheng Shu1,3, Rhett W Stout4
1School of Renewable Natural Resources, Louisiana State University Agricultural Center, Baton Rouge, LA 70803, USA.
Pharmaceutics
|August 29, 2024
概括
鲁布索西德形成纳米,以提高帕克利塔塞尔的溶解性和吸收性. 虽然这增加了88%的口服生物可用性,但为了增加全身循环,需要进一步抑制排泄.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 纳米技术 纳米技术
背景情况:
- 帕克利塔塞尔具有较差的水溶性和透性,限制了口服药物输送.
- 由于口服吸收率低,目前的帕克利塔塞尔配方需要静脉注射.
- 像帕克利塔克塞尔这样的流出基板在通过口服途径实现治疗生物可用性方面面临挑战.
研究的目的:
- 评估rubusoside,一种天然化合物,用于增强巴克利塔的口服生物可用性.
- 开发使用rubusoside的paclitaxel纳米细胞,以改善药物输送.
- 为了比较巴克利塔克塞尔纳米粒与常规的Taxol配方的口服生物利用性.
主要方法:
- 帕克利塔克塞尔用水溶液中的rubusoside制成纳米微粒.
- 使用动态光散射测量纳米粒的粒子大小.
- 在Sprague Dawley大鼠口服和静脉注射帕克利塔塞尔纳米塞尔和Taxol,以确定生物可用性.
主要成果:
- 由鲁布索西德形成的帕克利塔塞尔纳米粒达到6mg/mL的超和度.
- 纳米微粒的平均颗粒大小为4.7 ± 0.7 nm.
- 相对的口服生物利用率增加了88%,最大血度比Taxol高1.5倍.
结论:
- 鲁布索西德有效地将帕克利塔塞尔溶解成纳米,改善其口服生物利用性.
- 尽管有所改善,但绝对口服生物利用率仍然很低,这表明需要进一步的策略.
- 抑制排泄和/或第一通代谢可能会增强口服帕克利塔塞尔的输送.
相关概念视频
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