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NMITLI118RT+的磷脂络合作用:大鼠缺血性中风实现有益治疗效果的审慎治疗途径

Phospholipid complexation of NMITLI118RT+: way to a prudent therapeutic approach for beneficial outcomes in ischemic stroke in rats.

作者信息

Ahmad Hafsa, Arya Abhishek, Agrawal Satish, Samuel Sheeba Saji, Singh Sandeep Kumar, Valicherla Guru Raghavendra, Sangwan Neelam, Mitra Kalyan, Gayen Jiaur R, Paliwal Sarwesh, Shukla Rakesh, Dwivedi Anil Kumar

机构信息

a Division of Pharmaceutics , CSIR-Central Drug Research Institute , Lucknow , India.

b Division of Pharmacology , CSIR-Central Drug Research Institute , Lucknow , India.

出版信息

Drug Deliv. 2016 Nov;23(9):3606-3618. doi: 10.1080/10717544.2016.1212950. Epub 2016 Aug 12.

DOI:10.1080/10717544.2016.1212950
PMID:27685355
Abstract

Withania somnifera Dunal (Solanaceae) known as Ashwagandha, a popular plant of Indian origin is known to possess tremedous medicinal potential, often used as anti-inflammatory, anti-platelet, antihypertensive, hypoglycemic, hypolipidemic and adaptogenic candidate. Some of its chemotypes developed by CSIR, India includes NMITLI-101, NMITLI-118, NMITLI-128. In this study the investigators have attempted development of a phytosomal complex of NMITLI118RT + (standardized ethanolic extract of a new chemotype of W. somnifera Dunal.), its pharmaceutical characterization and evaluation of its neuro-protective potential against experimenal stroke in rats in continuation with their previous work in this area. The phytosomal complex (NIMPLC) was prepared by following a cohesive optimization design and was characterized on the basis of solubility, dissolution profile, FT-IR, DSC-TGA analysis, zeta potential, physical stability, forced degradation and photolytic degradation. Results were suggestive of a pharmaceutically acceptable formulation. NIMPLC was taken up further for biological evaluation using the middle cerebral artery occlusion (MCAO) model in rats. It could be demonstrated that the beneficial effects of NMITLI118RT + could be augmented by NIMPLC in 1 h pre and 6 h post treatment as was evident from reduction in MDA levels, increment in GSH levels, reduction in neurological deficit (ND) scores and reduction in infarct size. The study could successfully demonstrate the beneficial effects of NIMPLC in brain function restoration following stroke.

摘要

印度人参(Withania somnifera Dunal,茄科),是一种源自印度的常见植物,具有巨大的药用潜力,常被用作抗炎、抗血小板、抗高血压、降血糖、降血脂和适应原性药物。印度科学与工业研究理事会(CSIR)开发的一些化学型包括NMITLI - 101、NMITLI - 118、NMITLI - 128。在本研究中,研究人员延续其在此领域之前的工作,尝试开发NMITLI118RT +(一种新化学型印度人参的标准化乙醇提取物)的植物脂质体复合物,对其进行药学表征,并评估其对大鼠实验性中风的神经保护潜力。植物脂质体复合物(NIMPLC)通过遵循连贯的优化设计制备,并根据溶解度、溶出曲线、傅里叶变换红外光谱(FT - IR)、差示扫描量热法 - 热重分析(DSC - TGA)、zeta电位、物理稳定性、强制降解和光解降解进行表征。结果表明该制剂在药学上是可接受的。使用大鼠大脑中动脉闭塞(MCAO)模型对NIMPLC进行进一步的生物学评估。可以证明,在治疗前1小时和治疗后6小时,NIMPLC可增强NMITLI118RT +的有益作用,这从丙二醛(MDA)水平降低、谷胱甘肽(GSH)水平升高、神经功能缺损(ND)评分降低和梗死面积减小中明显看出。该研究成功证明了NIMPLC在中风后脑功能恢复中的有益作用。

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