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Brain delivery of baclofen as a hydrophilic drug by nanolipid carriers: Characteristics and pharmacokinetics evaluation

Ghasemian, E. ; Vatanara, A. ; Navidi, N. ; Rouini, M.R. ;
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    Formulation of baclofen in lipid-based nanoparticles may be helpful to overcome its difficulties in order to reach the site of action in the CNS. This study reports production, characterization and pharmacokinetics evaluation of baclofen loaded lipid nano-carriers. Lipid nano-carriers containing baclofen were prepared by using double emulsion solvent evaporation method and physicochemical characteristics of prepared nanoparticles were evaluated. The selected formulation was administered on rat model to be compared with an aqueous drug solution. Plasma and brain concentrations of drug and pharmacokinetics parameters were compared. Nanostructured lipid carriers (NLC) formulation showed better physicochemical properties than solid lipid nanoparticles (SLNs). Also, the formulation of baclofen by NLC increased the half-life of drug in plasma and brain up to 10 and 1.5 times respectively compared to the solution formulation. Results revealed a more significant and prolonged effect of baclofen-NLC in comparison with baclofen solution in both plasma and brain mediums that emphasize and prove theories on the formulation of hydrophilic drug in NLCs can be a solution for target drug delivery to the brain.


  • 주제어

    Baclofen .   NLC .   Sustained release .   Brain delivery .   Spasm.  

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