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首页> 外文期刊>Journal of Pharmacy and Pharmaceutical Sciences >Evaluation of Brain Targeting and Mucosal Integrity of Nasally Administrated Nanostructured Carriers of a CNS Active Drug, Clonazepam
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Evaluation of Brain Targeting and Mucosal Integrity of Nasally Administrated Nanostructured Carriers of a CNS Active Drug, Clonazepam

机译：中枢神经系统活性药物氯硝西am经鼻给药的纳米结构载体的脑靶向性和粘膜完整性评估

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PURPOSE: The aim of the study was to target clonazepam, a CNS active drug, to the brain through the non-invasive intranasal (in) route using of nanocarriers with proven safety METHOD: in clonazepam nanocarriers were prepared by mixing isopropyl myristate, Tween 80, Cremophor EL or lecithin, polyethylene glycol 200, propylene glycol or ethanol in different ratios with water. in-vitro characterization of the nanocarriers was done by various methods including: polarized light microscopy, particle size determination, viscosity measurements and drug release studies. in-vivo study comparing intranasal and intravenous administration was performed. The drug targeting efficiency (DTE %) and direct nose to brain transport percentage (DTP %) were calculated and nasal integrity assessment was carried out. RESULTS: The obtained formulae had particle size below 100 nm favoring rapid direct nose to brain transport and the time for 100% drug release (T100%) depended on systems composition. Plasma Tmax of clonazepam nanostructured carriers varied from 10-30 min., while their brain Tmax did not exceed 10 min, in comparison with 30 min for iv solution. Although there was no significant difference (p>0.05) between the plasma AUC0-∞ of the different tested nanocarriers and intravenous one, the increase in brain AUC 0 -∞ of different nasal formulations in comparison to that of iv administration (3.6 -7.2 fold) confirms direct nose to brain transport via olfactory region. Furthermore, DTE and DTP% confirmed brain targeting of clonazepam following intranasal administration. CONCLUSION: The results confirmed that intranasal nanocarriers were proved to be safe alternative for iv clonazepam delivery with rapid nose to brain transport. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.
机译：目的：本研究的目的是通过使用经验证的安全性的纳米载体，通过无创性鼻内（途中）途径将中枢神经系统活性药物氯硝西target靶向大脑，方法：在氯硝西am中，通过混合肉豆蔻酸异丙酯，吐温80制备纳米载体，不同比例的Cremophor EL或卵磷脂，聚乙二醇200，丙二醇或乙醇与水的比例。纳米载体的体外表征通过多种方法完成，包括：偏振光显微镜，粒度测定，粘度测量和药物释放研究。进行了鼻内和静脉内给药比较的体内研究。计算药物靶向效率（DTE％）和直接鼻-脑转运百分比（DTP％），并进行鼻腔完整性评估。结果：所获得的配方的粒径小于100 nm，有利于鼻腔到大脑的快速直接转运，并且100％药物释放的时间（T100％）取决于系统组成。氯硝西am纳米结构载体的血浆Tmax在10至30分钟之间变化，而其脑部Tmax不超过10分钟，而静脉注射液的血浆Tmax则不超过30分钟。尽管不同被测试的纳米载体的血浆AUC0-∞与静脉内载体的血浆AUC0-∞没有显着差异（p> 0.05），但是与静脉内给药相比，不同鼻腔制剂的脑AUC0-∞的增加（3.6 -7.2倍） ）确认通过嗅觉区域将鼻子直接运送至大脑。此外，经鼻内给药后，DTE和DTP％证实了氯硝西brain的脑靶向性。结论：结果证实鼻内纳米载体被证明是静脉输注氯硝西am的安全替代品，鼻腔快速转运至脑部。本文对发布后审查开放。已注册的读者（请参阅“针对读者”）可以通过在问题目录页面上单击摘要来发表评论。

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