抗坏血酸系缚聚合纳米颗粒对利瓦斯汀脑运输的体内研究。

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery Pub Date : 2023-01-01 DOI:10.2174/1567201819666220516093425

Kavita R Gajbhiye, Vandana Soni

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引用次数: 1

摘要

本研究的目的是观察抗坏血酸移植的聚乳酸-聚乙二醇纳米颗粒(PLGA-b-PEG NPs)是否可以通过脉络膜丛钠依赖性维生素C转运体2 (SVCT2转运体)提高利瓦斯汀(RSM)到大脑的携带或运输能力。利用红外光谱和核磁共振氢谱对PLGA-b-PEG共聚物进行表征。方法:采用纳米沉淀法制备PLGA-b-PEG纳米粒子。为了促进SVCT2介导的抗坏血酸(Asc)进入大脑的运输，将可接受大小、多分散性和药物负荷的PLGA-b-PEG NPs与抗坏血酸(PLGA-b-PEG-Asc)结合。与PLGA-b-mPEG NPs相比，抗坏血酸对NPs的表面功能化显著提高了SVCT2表达NIH/3T3细胞对NPs的细胞摄取。采用桡臂迷宫实验和东莨菪碱致遗忘大鼠乙酰胆碱酯酶(AChE)活性评价其体内药效学效果。结果:体内药效学试验显示，载药PLGA-b-PEG-Asc NPs比游离药物具有更大的治疗和持续活性，并且PLGA-b-mPEG NPs对大脑具有更大的作用。结论:因此，研究结果表明，使用抗坏血酸移植的PLGA-b-PEG NPs将生物活性物质输送到大脑是一种潜在的策略。

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An In vivo Investigation of Ascorbic Acid Tethered Polymeric Nanoparticles for Effectual Brain Transport of Rivastigmine.

Introduction: The goal of this study was to see if ascorbic acid grafted polylactic glycolic acid-b-polyethylene glycol nanoparticles (PLGA-b-PEG NPs) might boost the carrying or transport capacity of rivastigmine(RSM) to the brain via choroid plexus Sodium-dependent vitamin C transporter 2 (SVCT2 transporters). The IR and 1H NMR, were used to characterise the PLGA-b-PEG copolymer.

Methods: Nanoprecipitation method was used to make PLGA-b-PEG NPs. To promote SVCT2- mediated transportation of ascorbic acid (Asc) into the brain, PLGA-b-PEG NPs of acceptable size, polydispersity, and drug loading were bound with ascorbic acid (PLGA-b-PEG-Asc). When compared to PLGA-b-mPEG NPs, the surface functionalization of NPs with ascorbic acid dramatically improved the cellular uptake of NPs in SVCT2 expressing NIH/3T3 cells. Radial Arm Maze Test, and Acetylcholinesterase (AChE) activity in scopolamine-induced amnetic rats were used to assess in vivo pharmacodynamic effectiveness.

Results: In vivo pharmacodynamic tests revealed that drug loaded PLGA-b-PEG-Asc NPs had much greater therapeutic and sustained activity than free drugs, and PLGA-b-mPEG NPs to the brain.

Conclusion: As a consequence, the findings revealed that using ascorbic acid grafted PLGA-b-PEG NPs to deliver bioactives to the brain is a potential strategy.

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来源期刊

Current drug delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.10

自引率

4.20%

发文量

170

期刊介绍： Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.