实现零级控制的通过双离子H键在补丁中的竞争性双离子H键通过皮肤间的药物透
Shuai Zhang1, Quanzhi Zhang1, Runmei Xu1
1Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning 110016, China.
International journal of pharmaceutics
|September 13, 2023
概括
这项研究引入了一种通过稳定粘合剂中的药物度来稳定透皮药物递送系统 (TDDS) 的新策略. 这种方法使零顺序控制的药物从贴片中释放出来,克服了药物输送的先前挑战.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 透皮药物递送系统 (TDDS) 提供可控药物递送,但从药物粘合剂贴片中实现零顺序释放仍然是一个重大挑战.
- 现有的TDDS经常与一致的药物释放动力学作斗争,影响治疗疗效和患者遵守.
研究的目的:
- 开发一种新的策略,以实现通过皮肤贴片实现零顺序控制的药物皮肤输送.
- 通过使用度依赖的竞争性相互作用,稳定粘合剂矩阵内的药物度.
- 评估基 (HP) 和聚二甲基乙烯酸 (EA) 粘合剂系统的有效性,以控制模型药物的释放.
主要方法:
- 使用克隆 (CLO) 和格拉尼塞特龙 (GRA) 作为具有高皮肤透性的模型药物.
- 纳入聚二甲基乙烯酸 (EA) 作为辅助剂与基 (HP) 粘合剂相互作用.
- 进行的药物释放,皮肤透和药理动力学研究.
- 使用FT-IR,1H NMR和XPS进行分子相互作用的特征.
- 采用动态模拟和分子对接来阐明竞争性相互作用机制.
主要成果:
- 惠普-EA粘合剂系统表现出对CLO和GRA皮肤透的良好零顺序适配 (r值为0.994和0.998).
- 对CLO补丁的药理动力学研究显示,持续的平原阶段持续约52小时,而不会改变度-时间曲线 (AUC) 下的面积.
- 机制研究显示,EA充当缓冲剂,稳定释放的中性药物物种度.
结论:
- 开发的透皮药物递送系统有效地实现了零顺序控制的药物皮肤递送.
- 度依赖的竞争性相互作用策略扩大了对TDDS分子机制的理解.
- 这种方法有望促进通过皮肤贴片的零顺序药物输送的发展.
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