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用于帕金森病治疗的载盐酸司来吉兰纳米脂质载体鼻腔给药系统的研发与表征

Development and Characterization of Nasal Delivery of Selegiline Hydrochloride Loaded Nanolipid Carriers for the Management of Parkinson's Disease.

作者信息

Mishra Neeraj, Sharma Sawarni, Deshmukh Rahul, Kumar Anoop, Sharma Ruchika

机构信息

Department of Pharmaceutics, ISF College of Pharmacy, Ghal Kalan, Ferozpur, G.T. Road Moga-142001, Punjab, India.

Department of Pharmacology, MRSPTU, Bathinda, India.

出版信息

Cent Nerv Syst Agents Med Chem. 2019;19(1):46-56. doi: 10.2174/1871524919666181126124846.

Abstract

INTRODUCTION

Parkinson's Disease (PD) is one of the most common age-related neurodegenerative disorders which is marked with the loss of dopaminergic neurons. The present study performed on the nose to brain delivery of selegiline hydrochloride loaded nano lipid carrier, suggests that the nasal route is a good mean of targeting the drug directly into the brain.

METHODS AND MATERIALS

Nanostructured lipid carriers were prepared by using hot homogenization. Selegiline hydrochloride loaded NLCs and rotenone treatment were given at a dose of 10 mg/kg administered from 14th day to 28th day. Behavioral parameters were determined at 7th, 14th, 21st and 28th day. On the 28th day, animals were sacrificed for biochemical estimation.

RESULTS

The optimized drug loaded NLC formulation has shown 93±5.25% entrapment efficiency and 51.96% loading capacity. Optimized NLCs formulation has shown 70% release within 10 hours and after that, the release of the drug is sustained up to 22 hours (97%). Pharmacological action of the drug was found to restore the behavioral parameters in rotenone-induced rats.

CONCLUSION

Nano Lipid Carrier (NLCs) therapeutics has emerged as a prominent method for the treatment of Parkinson's Disease (PD) as it offers targeted delivery and enhances the therapeutic efficacy of neurotherapeutics. It is concluded from the studies that, Selegiline HCl loaded nano lipid carrier which was administered through nasal route has the potential to be used in the management therapy of Parkinson's disease.

摘要

引言

帕金森病(PD)是最常见的与年龄相关的神经退行性疾病之一,其特征是多巴胺能神经元丧失。本研究对载有盐酸司来吉兰的纳米脂质载体进行鼻脑给药,结果表明鼻内途径是将药物直接靶向输送到大脑的良好途径。

方法与材料

采用热均质法制备纳米结构脂质载体。从第14天至第28天,以10mg/kg的剂量给予载有盐酸司来吉兰的纳米脂质载体和鱼藤酮处理。在第7天、第14天、第21天和第28天测定行为参数。在第28天,处死动物进行生化评估。

结果

优化后的载药纳米脂质载体配方的包封率为93±5.25%,载药量为51.96%。优化后的纳米脂质载体配方在10小时内释放70%,之后药物持续释放长达22小时(97%)。发现该药物的药理作用可恢复鱼藤酮诱导大鼠的行为参数。

结论

纳米脂质载体(NLCs)疗法已成为治疗帕金森病(PD)的一种重要方法,因为它提供靶向递送并提高神经治疗药物的疗效。研究得出结论,经鼻给药的载有盐酸司来吉兰的纳米脂质载体有潜力用于帕金森病的管理治疗。

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