The spray-dried mucoadhesive microparticles of rizatriptan with chitosan and carbopol in migraine

Abstract

Background The traditional oral formulation for migraine treatment has the drawbacks of first-pass metabolism, plasma-protein binding, and poor blood–brain-barrier penetration. This study was conducted to establish the nasal route of administration for rizatriptan formulations in migraine. Materials and methods Rizatriptan mucoadhesive microparticles were synthesized by spray-drying and evaluated for infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. The ex vivo study was done with Franz’s diffusion cell using goat nasal mucosa. The in vivo study was performed on the Albino rat’s nasal route for determining drug concentration by high-performance liquid chromatography analysis in brain tissue at single-point evaluation. Result The microparticles were of optimum size with no drug–polymer interaction in infrared spectroscopy and differential scanning calorimetry. Scanning electron microscopy exhibited the morphology of spherical or ellipsoid microparticles with efficient drug entrapment. The percentage of drug permeability for chitosan microparticles was 76.53–91.09 and for carbopol microparticles was 78.49–92.25 in the ex vivo permeability study. In vivo studies showed that drug concentrations of 126.46–148.50% for chitosan batches and 152.83–165.04% for carbopol batches were superior to controls. Conclusion Ex vivo permeability study revealed drug-permeation patterns as high as 91.09±0.03% for RCH3 formulation and 92.25±0.2% for RC3 formulation. In in vivo study formulation, RCH3 displayed a drug concentration of 132.22±8.32% and RC3 showed 159.46±4.05% over the control batch, which is conclusive for improved drug delivery of rizatriptan through mucoadhesive microparticles for the nose-to-brain targeting in migraine.