Rational design and characterisation of intranasal gel incorporating eletriptan HBr-loaded solid lipid nanoparticles for enhanced brain delivery in migraine

Eletriptan HBr-loaded solid lipid nanoparticles (ESLN) were designed for brain delivery by circumventing first-pass metabolism and the blood-brain barrier. The formulation combines biocompatible polymers with the permeability-enhancing properties of lipids. A central composite design was employed to optimize formulation variables to achieve ESLN with optimal physicochemical characteristics. The optimized ESLN showed a mean particle size of 257.4 ± 106.3 nm, zeta potential of -23.3 ± 4.25 mV, and entrapment efficiency of 71.77 ± 0.58%. SEM reveals smooth-surfaced, spherical nanoparticles. In situ nasal gel of ESLN was optimized using a 3 2 full factorial design. The gel exhibited a gelation temperature of 34.7 ± 0.6 °C and a gelation time of 68 ± 4.58 s, with a viscosity ranging from 120 ± 8.6 cPs at 25 °C to 11,230 ± 255 cPs at 35 °C. Ex vivo studies demonstrated 65.29 ± 3.12% cumulative Eletriptan HBr (EBr) permeation from the ESLN gel, compared to 51.69 ± 3.30% from the plain gel over 24 h. Brain biodistribution studies in Wistar rats demonstrated enhanced brain exposure of EBr following administration of the ESLN gel, with a Cmax of 1542.284 ng/g and an AUC0-∞ of 22,910.8 ng·h/g, compared with the plain EBr-loaded gel. Histology of the brain and nasal mucosa confirmed the formulation's safety.

Abstract from PubMed (PMID 42992789). This entry was added automatically by our daily literature monitor because it matches the topics we follow; read the full paper at the original source.