使用聚合物作为晶体抑制剂来防止罗提古丁贴片的结晶
Qiantong Liu1, Xing Li1, Bo Liu1
1School of Chemical Engineering, Dalian University of Technology, Dalian 116024, China.
Pharmaceutics
|May 25, 2024
概括
这项研究使用聚合物作为晶体抑制剂开发了稳定的罗提古丁 (ROT) 补丁. 使用Soluplus和TPGS的高度ROT防止了90天的结晶,改善了透皮输送.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 罗提古丁 (ROT) 贴片用于帕金森病治疗.
- 在补丁中ROT的结晶降低了稳定性和有效性.
- 聚合物可以作为晶体抑制剂来增强药物稳定性.
研究的目的:
- 用聚合物作为晶体抑制剂来增强罗提古丁 (ROT) 贴片的稳定性.
- 评估Poloxamer 188,Soluplus和TPGS在防止ROT结晶中的有效性.
- 评估晶体抑制剂对ROT的通过皮肤传递的影响.
主要方法:
- 使用Poloxamer 188,Soluplus和TPGS,配制具有不同药物负载 (20-80%w/w) 的ROT贴片.
- 扫描电子显微镜 (SEM) 和X射线衍射 (XRD) 用于结晶分析.
- 分子对接以阐明药物聚合物相互作用和结合稳定性.
- 在体外皮肤透研究以评估通过皮肤的影响.
主要成果:
- 80%ROT和Soluplus-TPGS的ROT贴片在室温下90天后没有结晶.
- 聚合物有效地阻碍了ROT晶体的形成,并减缓了结晶率.
- ROT-Soluplus-TPGS组合显示出最高的结合稳定性 (-5.3 kcal/mol).
- 补丁中的ROT度增加增加了累积透率,并减少了滞后时间.
结论:
- 聚合物,特别是Soluplus和TPGS,通过抑制结晶,显著提高ROT补丁的稳定性.
- 开发的ROT贴片表现出有希望的通过皮肤递送特征.
- 这项研究为设计稳定有效的透皮药物输送系统提供了宝贵的见解.
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