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通过吸入途径开发和描述pH值敏感的,通过吸入途径治疗肺纤维化的囊化脂体
Nourhan Elsayed1, Chee Wun How2, Jhi Biau Foo3
1School of Pharmacy, Faculty of Health & Medical Sciences, Taylor's University, Subang Jaya, Malaysia.
概括
泽伦 (ZER) 脂质体有效地将抗炎化合物传递给肺组织. 这种配方通过减少细胞迁移和纤维化标志物来治疗肺纤维化有望.
科学领域:
- 药理学 药理学是指药理学的学科.
- 纳米技术纳米技术
- 肺部医学 肺部医学
背景情况:
- 来自Zingiber Zerumbet的Zerumbone (ZER) 具有抗炎作用,但水溶性差限制了其使用.
- 目前,ZER在肺纤维化中的治疗潜力尚未被探索.
- 需要有针对性的输送系统来克服ZER在肺部应用中的可溶性限制.
研究的目的:
- 开发和描述pH敏感脂质体,以提高溶解度和基 (ZER) 的向输送.
- 为了研究ZER载脂质体在治疗肺纤维化模型中的有效性.
- 为了评估ZER脂质体的肺部沉积和细胞吸收.
主要方法:
- 使用油酸,DPPC和胆固醇,通过Box-Behnken设计进行优化,ZER被封装在pH敏感脂质体中.
- 分析了脂质体特征 (大小,PDI,泽塔潜力) 和ZER释放动力学.
- 在体外研究中评估了脂质体沉积 (级联冲击器,HPLC),细胞吸收 (MRC-5,A549细胞) 和抗纤维效应 (细胞迁移,纤维细胞标志物).
主要成果:
- 优化脂质体的平均直径为87.8nm,PDI为0.16,而zeta电位为-24mV.
- 在酸性条件下,ZER释放遵循零级动力学,在酸性条件下释放强化.
- 泽尔脂质体表现出有效的深肺传递,pH依赖的细胞吸收,减少细胞迁移,以及纤维素,MMP-2和α-SMA的下调.
结论:
- 对pH敏感的ZER脂质体提高了溶解度,并使肺纤维化治疗的向输送成为可能.
- 脂质体配方在体外有效降低了关键纤维细胞标记物和细胞迁移.
- ZER脂质体代表了肺纤维化治疗的有前途的治疗策略,需要进一步研究.
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