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Preclinical Explorative Assessment of Dimethyl Fumarate-Based Biocompatible Nanolipoidal Carriers for the Management of Multiple Sclerosis
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2018-01-22 00:00:00 , DOI: 10.1021/acschemneuro.7b00519 Pramod Kumar 1 , Gajanand Sharma 2 , Varun Gupta 3 , Ramanpreet Kaur 4 , Kanika Thakur 2 , Ruchi Malik 1 , Anil Kumar 3 , Naveen Kaushal 4 , Kaisar Raza 1
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2018-01-22 00:00:00 , DOI: 10.1021/acschemneuro.7b00519 Pramod Kumar 1 , Gajanand Sharma 2 , Varun Gupta 3 , Ramanpreet Kaur 4 , Kanika Thakur 2 , Ruchi Malik 1 , Anil Kumar 3 , Naveen Kaushal 4 , Kaisar Raza 1
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Multiple sclerosis (MS) is a neurodegenerative disease in which myelin sheath damage occurs due to internal and external factors. MS especially affects the young population. Dimethyl fumarate (DMF) is a promising agent for MS treatment, although it is associated with concerns such as poor brain permeation, multiple dosing, and gastrointestinal flushing. The present study attempts to evaluate the preclinical performance of specially designed DMF-based lipoidal nanoparticles in a cuprizone-induced demyelination model in rodents. The studies proved the efficacy of lipid-based nanoparticles containing DMF in a once-a-day dosage regimen over that of thrice-a-day plain DMF administration on crucial parameters like motor coordination, grip strength, mortality, body weight, and locomotor activity. However, neither blank lipid nor blank neuroprotective (vitamins A, D, and E) loaded nanoparticles were able to elicit any desirable behavioral response. Histopathological studies showed that the designed once-a-day DMF nanomedicines were well tolerated and rejuvenated the myelin sheath vis-à-vis the plain DMF thrice-a-day regimen. These findings provide proof of concept for a biocompatible nanomedicine for MS with tremendous promise for effective brain delivery and patient compliance on the grounds of a reduction in the dosage frequency.
中文翻译：
基于富马酸二甲酯的生物相容性纳米脂质载体在多发性硬化症治疗中的临床前探索性评估
多发性硬化症（MS）是一种神经退行性疾病，其中髓鞘鞘由于内部和外部因素而受损。MS尤其影响年轻人口。富马酸二甲酯（DMF）是一种有前途的MS治疗药物，尽管它与不良的脑部通透性，多次给药和胃肠道冲洗有关。本研究试图评估专门设计的基于DMF的脂质纳米颗粒在啮齿类动物中由铜氮酮诱导的脱髓鞘模型中的临床前性能。研究证明，每日两次剂量的含DMF的脂质基纳米颗粒的效果优于每日三次三次的普通DMF给药，在诸如运动协调性，抓地力，死亡率，体重和运动能力等关键参数上的功效。然而，空白脂质和空白神经保护剂（维生素A，D和E）均无法引发任何所需的行为反应。组织病理学研究表明，设计的每天一次的DMF纳米药物具有良好的耐受性，并能使髓鞘恢复活力相对于普通DMF每天三次的方案。这些发现为用于MS的生物相容性纳米药物提供了概念验证，并基于减少给药频率而为有效的脑部输送和患者依从性提供了广阔的前景。
更新日期：2018-01-22
中文翻译：
基于富马酸二甲酯的生物相容性纳米脂质载体在多发性硬化症治疗中的临床前探索性评估
多发性硬化症（MS）是一种神经退行性疾病，其中髓鞘鞘由于内部和外部因素而受损。MS尤其影响年轻人口。富马酸二甲酯（DMF）是一种有前途的MS治疗药物，尽管它与不良的脑部通透性，多次给药和胃肠道冲洗有关。本研究试图评估专门设计的基于DMF的脂质纳米颗粒在啮齿类动物中由铜氮酮诱导的脱髓鞘模型中的临床前性能。研究证明，每日两次剂量的含DMF的脂质基纳米颗粒的效果优于每日三次三次的普通DMF给药，在诸如运动协调性，抓地力，死亡率，体重和运动能力等关键参数上的功效。然而，空白脂质和空白神经保护剂（维生素A，D和E）均无法引发任何所需的行为反应。组织病理学研究表明，设计的每天一次的DMF纳米药物具有良好的耐受性，并能使髓鞘恢复活力相对于普通DMF每天三次的方案。这些发现为用于MS的生物相容性纳米药物提供了概念验证，并基于减少给药频率而为有效的脑部输送和患者依从性提供了广阔的前景。
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