A Development and Evaluation of Rizatriptan Benzoate-loaded Nanostructured Lipid Carriers for the Treatment of Migraine

Abstract

The aim is to develop and evaluate rizatriptan benzoate (RB) loaded nanostructured lipid carriers (NLCs) that might improve oral bioavailability. NLC was prepared using High-Speed Homogenization (HSH) coupled with the ultrasonication method. Process parameters were selected on basis of the trial-and-error method which is time for homogenization, speed of homogenization, and time for sonication. RB-NLC was evaluated on basis of particle size, %Entrapment Efficiency (EE), Zeta potential, Transmission electron microscopy (TEM), In-Vitro permeation study, and Ex-vivo permeation study. Confocal Laser Scanning Microscopy was performed to study the uptake of RB-NLC through M-Cells, and Peyer's Patches. RB-NLC dispersion was converted into free-flowing lyophilized powder using cryoprotectant which is trehalose and in vitro permeation study was performed. The batch of RB-NLC was evaluated and showed a particle size of 412.8 ± 1.15nm with 0.261 PDI and − 36.6mV zeta potential. It showed 84.26 ± 1.03% EE. TEM image showed a spherical shape and smooth surface area. In-Vitro and Ex-vivo studies showed 97.21 ± 0.36%CDR up to 22 hours & 61.02 ± 1.25%CDR up to 6 hours. Lyophilized powder showed 96.37 ± 0.36%CDR up to 22 hours. Based on the data we can conclude that RB-NLC increases the permeation and it may increase its Bioavailability (BA). Lyophilized powder of RB-NLC showed a sustained release pattern and it may reduce the dosing frequency of the drug.