Formulation and evaluation of nasal mucoadhesive microspheres of sumatriptan succinate.
The purpose of present research work was to develop mucoadhesive microspheres for nasal delivery with the aim to avoid hepatic first-pass metabolism, improve therapeutic efficacy and enhance residence time. For the treatment of migraine, hydroxypropyl methylcellulose (HPMC) K4M and K15M based microspheres containing sumatriptan succinate (SS) were prepared by spray-drying technique. The microspheres were evaluated with respect to the yield, particle size, incorporation efficiency, swelling property, in vitro mucoadhesion, in vitro drug release, histological study and stability. Microspheres were characterized by differential scanning calorimetry, scanning electron microscopy and X-ray diffraction study. It was found that the particle size, swelling ability and incorporation efficiency of microspheres increases with increasing drug-to-polymer ratio. HPMC-based microspheres show adequate mucoadhesion and do not have any destructive effect on nasal mucosa. On the basis of these results, SS microspheres based on HPMC may be considered as a promising nasal delivery system.
Jain
Snehal A
SA
Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur 425 405, Maharashtra, India.
Chauk
Dheeraj S
DS
Mahajan
Hitendra S
HS
Tekade
Avinash R
AR
Gattani
Surendra G
SG
D000268:Adhesiveness; D000281:Administration, Intranasal; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives; D008863:Microspheres; D008881:Migraine Disorders / Q000188:drug therapy; D009297:Nasal Mucosa / Q000378:metabolism; D017366:Serotonin Receptor Agonists; D018170:Sumatriptan / Q000008:administration & dosage*; D014662:Vasoconstrictor Agents
D017366:Serotonin Receptor Agonists; D014662:Vasoconstrictor Agents; D065347:Hypromellose Derivatives; D018170:Sumatriptan; D008747:Methylcellulose