通过形成水凝的微针策略增强西尔德纳菲尔酸盐的生物可用性,并与循环德克斯林复合剂相结合
Sulistiawati Sulistiawati1, Cindy Kristina Enggi1, Israini Wiyulanda Iskandar2
1Faculty of Pharmacy, Hasanuddin University, Makassar 90245, Indonesia.
International journal of pharmaceutics
|March 27, 2024
概括
这项研究开发了一种新型的微针贴片,用于通过皮肤传递西尔德纳菲尔酸盐 (SIL),改善生物可用性,避免第一通代谢,以有效治疗勃起功能障碍.
科学领域:
- 制药科学 制药科学
- 生物材料工程 生物材料工程
- 药物输送系统 药物输送系统
背景情况:
- 西尔德纳菲尔酸盐 (SIL) 在口服勃起功能障碍治疗中具有较差的溶解性和生物可用性.
- 口服SIL导致第一通代谢,并可能通过注射引起不适.
研究的目的:
- 开发一种新型的西尔德纳菲尔酸盐 (SIL) 通过皮肤递送系统.
- 为了增强SIL溶解性,生物可用性和治疗勃起功能障碍的非侵入性治疗.
主要方法:
- 制造含有药片容器的凝形成微针.
- 加入SIL-β-环氧氨酸纳入复合物以增强溶解性.
- 评估微针的特性,胀能力和体内生物可用性.
主要成果:
- 微针显示出高胀能力 (>400%) 和足够的机械性能可以穿透皮肤.
- 分子对接证实了在β-cyclodextrin中SIL封装的成功.
- 在体内研究显示,与口服SIL和Viagra®相比,相对生物利用率>100%.
结论:
- 开发的透皮微针系统为SIL输送提供了一个非侵入性,安全和有效的替代方案.
- 这种方法绕过了第一通代谢,显著增加了治疗勃起功能障碍的药物生物可用性.
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