通过口服途径使用基于Poly (δ-decalactone) 的纳米乳液减轻塞莱科西布心脏毒性
Saurabh Maru1, Jyoti Verma2, Carl-Eric Wilen3
1School of Pharmacy and Technology Management, SVKM's NMIMS, Babulde, Banks of Tapi River, Mumbai-Agra Road, Shirpur, Maharashtra 425405, India.
概括
这项研究开发了一种纳米乳液 (NE) 用于切莱科西布 (CLX),改善溶解度并降低心脏毒性. 聚甲 (δ-decalactone) NE增强了不易溶解药物的抗炎活性和生物利用性.
科学领域:
- 制药纳米技术 制药纳米技术
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 抗炎药物塞莱科克西布 (CLX) 的溶解性较差,需要高剂量,这与心脏毒性有关.
- 开发有效的口服配方来治疗像CLX这样的溶性较差的药物仍然是制药研究中的一个重大挑战.
研究的目的:
- 使用纳米乳液 (NE) 技术增强赛莱科西布 (CLX) 的可溶性和治疗疗效.
- 评估CLX载荷NE的抗炎活性,心脏安全性和药物动力学特征.
- 评估开发的基于聚-十甲的纳米乳液的长期稳定性.
主要方法:
- 通过纳米沉使用聚-δ-decalactone (PDL) 和mPEG-b-PDL的CLX的纳米乳液 (NE) 配方.
- 在体外表征包括尺寸,药物释放动力学和稳定性评估.
- 在口服后对抗炎作用,心脏标志物和药理动学的体内评估.
主要成果:
- 成功准备了CLX载荷NE,球形大小小小于100nm,药物负荷高.
- 在体外持续释放药物,大约90%的CLX在96小时内释放.
- 与市场配方相比,观察到显著的抗炎活性和心脏标记物体内减少,增加了CLX保留时间.
结论:
- 基于Poly (δ-decalactone) 的纳米乳液显著改善了赛莱科西布 (CLX) 的生物可用性和抗炎疗效,同时减轻了心脏毒性.
- 开发的NE为难溶性药物提供了一个有前途的口服输送系统,显示出优异的长期存储稳定性.
- 纳米乳液技术为增强现有药物的治疗特性和开发难溶性化合物的新配方提供了一个可行的策略.
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