Development and Characterization of Gastro-Retentiv Blend Microparticles of Sumatriptan: Design, Optimization, ex vivo, and in vitro Evaluation for Oral Drug Delivery

gastro-retentive blend microparticles of sumatriptan

  • Mitra Jelvehgari Faculty of pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
  • Sara Salatin Faculty of pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
  • Pouya Darvishi Faculty of pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

Abstract

Objective: Sumatriptan (ST) is a 5-hydroxytryptamine receptor agonist commonly used 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 improve the therapeutic efficacy of orally administered ST.

Materials and Methods: The ST microparticles were prepared by the ionotropic gelation method 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 mucoadhesive strength, 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 in vitro drug release was extended for more than 8 h.

Conclusion: Therefore, it may be concluded that the gastro-retentive ST microparticles have promising properties and therefore, management of migraine in a better manner is expected with this formulation.

Keywords: Sumatriptan, Sodium alginate, Chitosan, Carbopol 934P, Mucoadhesive, Oral drug delivery.

Published
2020-11-26
Section
Original Article