Abstract
Background:
Sumatriptan (ST) is a selective serotonin receptor agonist with activity at the 5-HT₁B/1D receptor subtypes and is widely used for the acute treatment of migraine. However, its therapeutic effectiveness following oral administration is limited by a short elimination half-life of approximately 2 h and low oral bioavailability of about 15%.
Objective:
The objective of this study was to prepare and evaluate an intranasal mucoadhesive spanlastic nanovesicular (MSNV) gel of sumatriptan (ST) to enhance nasal residence time, overcome the limitations associated with the drug’s low oral bioavailability, and improve its potential for migraine management.
Methods:
ST-loaded spanlastic nanovesicles (SNVs) were prepared by the ethanol injection method and evaluated for particle size, polydispersity index (PDI), entrapment efficiency (EE%), and in vitro drug release. The optimized formulation (F8) was incorporated into different concentrations of mucoadhesive gelling polymer (Carbopol 934) to prepare mucoadhesive nanovesicular gels. The gels were evaluated for pH, drug content, viscosity, mucoadhesive force, and in vitro drug release. The selected formulation was further characterized by Fourier-transform infrared spectroscopy (FTIR) and ex vivo permeation studies.
Results:
F8 exhibited a particle size of 119.4± 0.82 nm, PDI of 0.252± 0.005, EE of 93.24%± 2.443, and approximately 93.2%±1.08 drug release within 4 h. MF1, containing 0.5% Carbopol® 934, showed favorable characteristics, with a pH of 5.4 ±0.13, drug content of 97±1.11%, mucoadhesive force of 0.235±0.007 N, approximately 95±1.21% drug release, and 94±1.27% ex vivo permeation within 4 h. FTIR analysis revealed no significant interaction between ST and the formulation excipients.
Conclusion:
Based on the findings of this study, the optimized ST-loaded MSNV gel represents a promising intranasal delivery system for ST, with the potential to overcome its poor oral bioavailability, prolong nasal residence time, and provide a rapid therapeutic response.
| Intend to be published in the IJPS ? | NO |
|---|---|
| Has the manuscript been published | not published |
