| Objective: Sumatriptan (ST) is a 5-hydroxytryptamine receptor agonist commonly suggested in the
treatment of migraine and cluster headaches. However, the bioavailability of ST is generally poor because of
the first-pass metabolism. The present work was undertaken to formulate gastro-retentive microparticles
of ST due to enhance the pharmaceutical effect of orally administered ST.
Materials and Methods: The ST microparticles were fabricated via the ionotropic gelation technique using
sodium alginate (SA) and different ratios of mucoadhsive polymers, namely, chitosan (CS), and carbopol
934P (CP). The developed microparticles were characterized by the production yield, drug loading,
entrapment efficiency, size, differential scanning calorimetry (DSC), swelling index, floating capacity, ex
vivo mucoadhesion effect, and in vitro drug release.
Results: The best formulations (F2 and F’2) exhibited satisfactory physicochemical characteristics. The ST
microparticles were detected to be in a micrometer size range. The microparticles exhibited very good
percentage of mucoadhesion compared with the SA microparticles. The prepared microparticles had a
slower release pattern than the commercial tablet (P<0.05) and the drug release was extended for 8 h.
Conclusion: It may be concluded that the gastro-retentive ST microparticles have promising properties
and therefore, this formulation is expected to improve migraine management in a better manner. |