Targeted SLNs for management of HIV-1 associated dementia. (August 2015)

• Record Type: Journal Article
• Authors: Rai, Ankit; Jain, Ankit; Jain, Ashish; Jain, Aviral; Pandey, Vikas; Chashoo, Gousia; Soni, Vandana; Sharma, P. R.
• Is Part Of: Drug development and industrial pharmacy. Volume 41:Number 8(2015:Aug.)
• Page Start: 1321
• Page End: 1327
• Publication Date: 2015-08
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.3109/03639045.2014.948453
• Languages: English
• ISSNs: 0363-9045

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context</italic>: HIV-1 associated dementia (HAD) is an evolving disease in the category of neurological disorders.</p> <p> <italic>Objective</italic>: Nifedipine-loaded solid lipid nanoparticles (SLNs) were developed and coated with Tween 80 to facilitate enhanced brain drug delivery for the treatment of HAD.</p> <p> <italic>Materials and methods</italic>: SLNs were prepared using solvent injection method. Lipids consisted of tristearin, hydrogenated soya phosphatidylcholine (HSPC) (1.5:1 <italic>w/w</italic>). Nifedipine was model drug in this study. Tween 80 (0.5% <italic>v/v</italic>) was taken as key modulator. SLNs were characterized for particle shape, size, zeta potential, entrapment efficiency, <italic>in vitro</italic> drug release, DNA fragmentation, cytotoxicity potential and <italic>in vivo</italic> studies.</p> <p> <italic>Results</italic>: The SLNs (plain and coated) were found to be in nanometric in size (∼120 nm) with more than 70% entrapment efficiency. <italic>In vitro</italic> drug release profile reflected sustained release up to 48 h. Tween 80-coated SLNs showed higher percentage of DNA fragmentation <italic>in vitro</italic> and enhanced cell viability in sulforhodamine assay (rat cortical cells) as compared to plain drug and uncoated SLNs due to facilitated uptake of SLNs and reversal of P-gp efflux by virtue of Tween 80. Biodistribution study performed on vital organs, i.e. brain, heart, liver, spleen, lungs and kidney showed increased accumulation of Tween 80-coated SLNs in the brain.</p> <p> <italic>Discussion and conclusion</italic>: Tween 80 enhanced localization of SLNs in the brain as compared to uncoated SLNs. This approach can be employed effectively to transport chemotherapeutics across the BBB for management of HIV-1 associated dementia and other ailments.</p> </abstract>