Lyotropic liquid crystalline nanoparticles of morin: An approach to improve pharmacokinetics and brain disposition in rats via nose-to-brain pathway

IF 4.2 2区 医学 Q2 MEDICINE, RESEARCH & EXPERIMENTAL
Dhrumi Patel M-Pharm, Sarika Wairkar PhD
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引用次数: 0

Abstract

Morin (MOR) is a potent neuroprotective agent possessing exceptional antioxidant abilities. The significant challenges associated with MOR delivery are poor solubility and low permeability. The present work aims to develop nasal delivery of MOR using lyotropic liquid crystalline nanoparticles (LLCs). MOR LLCs were prepared via the hydrotrope method, and 3-factor, 2-level factorial design was chosen for optimization. The results indicated MOR LLCs exhibited cubic vesicular structure, were non-toxic to nasal mucosa, and depicted sustained in vitro release. Pharmacokinetic studies showed MOR LLCs resulted in 1.53-fold and 1.42-fold enhancement in area under the curve than plain MOR oral and nasal groups. The relative drug targeting efficiency and relative direct transport percentage were 1.99-fold and 1.14-fold higher for MOR LLCs than plain nasal MOR, representing efficient brain targeting via olfactory pathways. Nasal administration of MOR LLCs enhances brain targeting and offers a self-administration option for prolonged utilization to alleviate neurological conditions.

Abstract Image

莫里素溶性液晶纳米颗粒:一种通过鼻-脑途径改善大鼠药代动力学和脑倾向的方法
桑里素(Morin, MOR)是一种有效的神经保护剂,具有特殊的抗氧化能力。与MOR输送相关的重大挑战是溶解度差和渗透率低。目前的工作旨在利用溶性液晶纳米颗粒(LLCs)开发经鼻给药MOR。采用水相法制备MOR llc,采用3因素、2水平析因设计进行优化。结果表明,MOR llc具有立方囊泡结构,对鼻黏膜无毒,体外释放持续。药代动力学研究显示,与普通MOR口服组和鼻组相比,MOR llc组的曲线下面积增加了1.53倍和1.42倍。与普通鼻腔MOR相比,MOR LLCs的相对药物靶向效率和相对直接转运率分别高出1.99倍和1.14倍,表明通过嗅觉途径有效靶向大脑。鼻给药MOR llc增强脑靶向性,并提供长期使用的自我给药选择,以缓解神经系统疾病。
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来源期刊
CiteScore
11.10
自引率
0.00%
发文量
133
审稿时长
42 days
期刊介绍: The mission of Nanomedicine: Nanotechnology, Biology, and Medicine (Nanomedicine: NBM) is to promote the emerging interdisciplinary field of nanomedicine. Nanomedicine: NBM is an international, peer-reviewed journal presenting novel, significant, and interdisciplinary theoretical and experimental results related to nanoscience and nanotechnology in the life and health sciences. Content includes basic, translational, and clinical research addressing diagnosis, treatment, monitoring, prediction, and prevention of diseases.
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