内鼻注射埃达拉纳米颗粒提高了其稳定性和大脑生物可用性
Yuan Lu1, Julie Tzu-Wen Wang2, Na Li3
1School of Cancer & Pharmaceutical Sciences, Faculty of Life Sciences & Medicine, King's College London, Franklin-Wilkins Building, London SE1 9NH, UK; Key Laboratory of Pharmaceutics of Guizhou Province, Guizhou Medical University, No. 9, Beijing Road, Yunyan District, Guiyang 550004, China.
概括
这项研究开发了新的纳米颗粒,用于ALS药物Edaravone (EDV) 的鼻入输送. 这种方法增强了大脑的药物输送,为肌缩性侧面硬化症患者提供了一个有前途的新治疗方案.
科学领域:
- 神经科学是一个神经科学.
- 纳米技术纳米技术
- 药理学 药理学是指药理学的学科.
背景情况:
- 埃达拉 (EDV) 是治疗ALS的抗氧化药物,但其临床使用因溶解性差和半衰期短而受到限制.
- 内静脉EDV需要住院治疗,目前的ALS治疗方法有限.
- 纳米颗粒药物输送和鼻到脑输送为改善药物稳定性和向大脑接入提供了潜在的解决方案.
研究的目的:
- 为了开发Edaravone (EDV) 装载的多分子乳糖合甘油酸 (PLGA) 纳米粒子 (NP-EDV) 用于鼻内注射.
- 评估NP-EDV的物理化学特性,稳定性和体外释放.
- 评估与静脉注射相比,内鼻输送的NP-EDV的体内药理学特征和大脑吸收.
主要方法:
- 纳米颗粒 (NP-EDV) 是使用纳米沉方法制成的.
- 描述包括形态,EDV负载,物理化学性质和保质期稳定性.
- 在BV-2细胞中进行了体外氧化应激降低和在小鼠体内药理动力学研究,使用光学成像和UPLC-MS/MS.
主要成果:
- NP-EDV成功配制了大约90nm大小和~3%的药物负载,显示稳定性长达30天.
- 在小鼠微质细胞系中,NP-EDV在减少H2O2诱导的氧化应激方面表现出有效性.
- 与静脉注射相比,NP-EDV的鼻内注射导致EDV在大脑中的度显著更高,持续时间更长.
结论:
- 这项研究介绍了Edaravone (EDV) 的第一个纳米颗粒配方,用于鼻到脑的输送.
- 鼻内NP-EDV提供了一种改善EDV的输送策略,增强大脑的生物可用性,并可能改善ALS治疗.
- 这种新的方法对ALS患者来说是有希望的,因为它克服了当前EDV管理的局限性.
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