Development of mucoadhesive in-situ nasal gel formulation for enhanced bioavailability and efficacy of rizatriptan in migraine treatment

Abstract

This research article focuses on the development of an in-situ nasal gel formulation for the antimigraine agent, Rizatriptan (RZT), to enhance its bioavailability and efficacy in treating migraine. The aim of the study was to overcome the challenges of rapid mucociliary clearance. Carbopol 934P (1–2 %w/v) was added to the primary solution, followed by HPMC K4M (0.4–1.2 %w/v). Different copolymers were tested, and HPMC K4M was chosen due to its compatibility with the other ingredients. The pH of all formulations was in the nasal pH range, and the drug content was above 97% in all batches. Gelling time varied from 1.3 to 8.6 sec, with low gelling time observed when viscosity and mucoadhesive strength were high. The results were analyzed using a statistical model with interactive and polynomial terms. The statistical analysis showed a good correlation between dependent and independent variables, with R2 values of 0.97758 and 0.948931 for viscosity and mucoadhesive strength, respectively. The Cmax of RZT in the brain was significantly higher (p < 0.05) via intra-nasal (340.27 ng) route as compared to the oral route and the same was the case for AUC. Finally, it was concluded that the RZT nasal in-situ gel system improves bioavailability compared with oral route and could provide fast action in migraine therapy.

Keywords

• Rizatriptan
• Mucoadhesive
• In-situ nasal gel
• Carbopol 934P
• HPMC K4M