通过脂质体封装增强ivermectin的细胞内吸收
Meryem Kocas1,2,3,4, Fumiyoshi Yamashita5,4, Tansel Comoglu6
1Faculty of Pharmacy, Department of Pharmaceutical Technology, Selcuk University, Selçuklu, Konya, 42130, Turkey.
脂质体封装通过增强细胞吸收和降低细胞毒性,显著改善ivermectin (IVM) 输送. 这种配方策略有望提高IVM对各种疾病的治疗效果.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 伊弗梅克丁 (IVM) 是一种抗寄生虫药物,具有潜在的抗病毒应用,但其不良的水溶性限制了生物可用性.
- 脂质体是有效的药物载体,增强溶解性,使向递送成为可能,并控制脂性药物的释放动力学.
研究的目的:
- 开发和评估ivermectin (IVM) 的脂质体配方,以改善其细胞吸收并减少细胞毒性.
- 为了比较体外细胞吸收和细胞毒性自由IVM与IVM载荷脂质体在Vero E6细胞.
主要方法:
- 通过乙醇注射方法,使用大豆酸胆,二醇酸胆,胆固醇和二甲基酸盐制备了IVM的脂质体配方.
- 脂质体的物理化学特性以前已经被表征;这项研究侧重于体外细胞吸收和细胞毒性测试.
- 使用Vero E6细胞来评估自由IVM和IVM载体脂质体的半最大细胞毒性度 (CC50) 和细胞吸收百分比.
主要成果:
- 脂质体封装显著增加了IVM细胞吸收,从13%到60%,相比之下,只有2%的自由IVM.
- 带有IVM的脂质体的半最大细胞毒性度 (CC50) 显著高于自由IVM (10微米) 的半最大细胞毒性度 (>110微米),表明毒性降低.
- 脂质体配方通过改善吸收和降低细胞毒性来增强IVM的治疗指数.
结论:
- 脂质体封装是一种可行的策略,可以克服艾弗梅克溶解性和生物可用性差的局限性.
- 这种方法增强了IVM的细胞传递,并降低了其固有的细胞毒性,为提高治疗疗效铺平了道路.
- 开发的脂质体IVM配方代表了治疗被忽视的热带疾病和潜在的病毒感染的有希望的进步.
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