4.7 Article

Stearic acid based, systematically designed oral lipid nanoparticles for enhanced brain delivery of dimethyl fumarate

Journal

NANOMEDICINE
Volume 12, Issue 23, Pages 2607-2621

Publisher

FUTURE MEDICINE LTD
DOI: 10.2217/nnm-2017-0082

Keywords

biodistribution; brain bioavailability; brain delivery; Caco-2 permeability; formulation optimization; fumaric acid ester; multiple sclerosis; NLCs; oral dosage; pharmacokinetics; QbD; SLNs

Funding

  1. UGC-National Fellowship [F./2014-15/NFO-2014-15-OBC-RAJ-8108/[SAIII/Website]]
  2. Central University of Rajasthan

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Aim: Dimethyl fumarate is a frequent prescription for the management of numerous neurological disorders. Despite immense promises, DMF is associated with various problems such as multiple dosing (2-3 oral doses daily) and lower brain permeability. Our aim was to enhance the oral bioavailability and increase the brain concentrations of dimethyl fumarate. Methods: Solid lipid nanoparticles were systematically formulated by optimizing the composition based on the desired attributes viz. particle size, entrapment efficiency and amount of drug released in 6 h. Results & conclusion: The developed system offered nanometric particle size with entrapment efficiency > 90%. Enhanced Caco-2 cells cellular uptake by optimized solid lipid nanoparticless with superior pharmacokinetic and higher brain biodistribution were observed.

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