Background: Sumatriptan succinate (SUT) is a potent drug used for relieving or ending
migraine and cluster headaches. SUT bioavailability is low (15%) when it is taken orally
owing to its gastric breakdown and bloodstream before reaching the target arteries.
Aim: The aim of the study was to enhance SUT bioavailability through developing an
intranasal transferosomal mucoadhesive gel.
Methods: SUT-loaded nanotransferosomes were prepared by thin film hydration method
and characterized for various parameters such as vesicle diameter, percent entrapment
efficiency (%EE), in vitro release and ex vivo permeation studies. The in-situ gels were
prepared using various ratios of poloxamer 407, poloxamer 188, and carrageenan and
characterized for gelation temperature, mucoadhesive strength, and rheological properties.
Results: The prepared transferosomes exhibited percent entrapment efficiencies (%EE) of
40.41±3.02 to 77.47±2.85%, mean diameters of 97.25 to 245.01 nm, sustained drug release
over 6 hours, and acceptable ex vivo permeation findings. The optimum formulae were
incorporated into poloxamer 407 and poloxamer 188-based thermosensitive in-situ gel using
carrageenan as a mucoadhesive polymer. Pharmacokinetic evaluation showed that the prepared
in-situ gel of SUT-loaded nano-transferosomes gave enhanced bioavailability, 4.09-
fold, as compared to oral drug solution.
Conclusion: Based on enhancing the bioavailability and sustaining the drug release, it can
be concluded that the in-situ gel of SUT-loaded nano-transferosomes were developed as
a promising non-invasive drug delivery system for treating migraine.