4.3 Article

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

Journal

CURRENT DRUG DELIVERY
Volume 20, Issue 7, Pages 961-977

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1567201819666220516093425

Keywords

Ascorbic acid; dementia; PEGylation; rivastigmine; targeted drug delivery system; brain

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The study aimed to investigate the potential of ascorbic acid grafted PLGA-b-PEG NPs in enhancing the transport of rivastigmine (RSM) to the brain via SVCT2 transporters. Results revealed that using ascorbic acid grafted PLGA-b-PEG NPs is a potential strategy for delivering bioactives to the brain.
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 H-1 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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