Journal
NANOMEDICINE
Volume 12, Issue 23, Pages 2607-2621Publisher
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
- UGC-National Fellowship [F./2014-15/NFO-2014-15-OBC-RAJ-8108/[SAIII/Website]]
- 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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