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新型阴离子聚合物作为抗阿尔茨海默病药物中枢神经系统递送载体

Novel anionic polymer as a carrier for CNS delivery of anti-Alzheimer drug.

作者信息

Jakki Satya Lavanya, Ramesh Yasam Venkata, Gowthamarajan K, Senthil V, Jain Kunal, Sood Sumeet, Pathak Deepa

机构信息

a Department of Pharmaceutics , JSS College of Pharmacy, Off Campus J.S.S. University , Mysore, Udhagamandalam, Tamil Nadu , India.

b Scientific Writer, Novartis Healthcare Pvt. Ltd , Hyderabad, Andhra Pradesh , India.

出版信息

Drug Deliv. 2016 Nov;23(9):3471-3479. doi: 10.1080/10717544.2016.1196767. Epub 2016 Jun 29.

Abstract

Natural and plant-based polymers could be used for control release of drugs and also helps in targeting drug to the site of action. The main objective of present work was to check the feasibility of plant-based, namely, mango gum polymeric nanoparticles (NPs) as a carrier for central nervous system (CNS) delivery using model drug donepezil (DZP). The NPs were prepared by modified ionic gelation method and emulsion cross-linking method. Zeta sizer results showed that the diameter of NPs was about 90-130 nm. The polymeric DZP-loaded NPs were almost spherical in shape, as revealed by transmission electron microscopy (TEM). On increasing concentration of NPs suspension from 50 μg/ml to 5000 μg/ml there was no significant increase in % hemolysis. In vivo studies showed that brain targeting was achieved. So on the basis of above results, the extracted water soluble fraction of mango gum is a suitable candidate for brain delivery in the form of nanoformulations.

摘要

天然和植物基聚合物可用于药物控释,还有助于将药物靶向输送到作用部位。本研究的主要目的是检验以植物为基础的芒果胶聚合物纳米颗粒(NPs)作为使用模型药物多奈哌齐(DZP)进行中枢神经系统(CNS)给药载体的可行性。通过改良离子凝胶法和乳液交联法制备了纳米颗粒。Zeta粒度分析仪结果显示,纳米颗粒的直径约为90 - 130纳米。透射电子显微镜(TEM)显示,负载聚合物的DZP纳米颗粒几乎呈球形。将纳米颗粒悬浮液浓度从50μg/ml增加到5000μg/ml时,溶血百分比没有显著增加。体内研究表明实现了脑靶向。因此,基于上述结果,提取的芒果胶水溶性部分是纳米制剂形式脑递送的合适候选物。

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