methylcellulose and Migraine-Disorders

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.

Topics: Adhesiveness; Administration, Intranasal; Hypromellose Derivatives; Methylcellulose; Microspheres; Migraine Disorders; Nasal Mucosa; Serotonin Receptor Agonists; Sumatriptan; Vasoconstrictor Agents

We have successfully obtained sumatriptan transdermal systems with different polymer compositions: methyl cellulose (MC), polyvinyl pyrrolidone (PVP) and a polyvinyl pyrrolidone (PVP)-polyvinyl alcohol (PVA) mixture. The systems contained 1,2-propylenglycol (MC) or sorbitol as a plasticizer (PVP and PVP-PVA), methacrylate copolymer as an adhesive agent, and an occlusive liner. Azone (5%, w/w) was incorporated into all the systems as a percutaneous enhancer. Transdermal systems are thin, transparent and non-adhesive when in a dry state. The permeation of sumatriptan succinate across pig ear skin was studied using the systems prepared. The formulation with MC polymer produced a statistically significant increment with respect to the PVP and PVP-PVA formulations (p < 0.05). Azone incorporation into the systems produced an increment in the sumatriptan flux values of all three transdermal systems with respect to those of the controls (p < 0.05). In addition, the application of iontophoresis to the wet methyl cellulose-Azone formulation produced a much higher increase of sumatriptan transdermal flux.

Topics: Administration, Cutaneous; Animals; Azepines; Chemistry, Pharmaceutical; Diffusion Chambers, Culture; Drug Carriers; Drug Compounding; Iontophoresis; Kinetics; Methylcellulose; Migraine Disorders; Permeability; Plasticizers; Polymers; Polymethacrylic Acids; Polyvinyl Alcohol; Povidone; Propylene Glycol; Serotonin Receptor Agonists; Skin; Skin Absorption; Sorbitol; Sumatriptan; Swine; Technology, Pharmaceutical; Tissue Adhesives; Vasoconstrictor Agents

Optimisation of novel cis- and trans-4-(substituted-amido)benzopyran-3-ol derivatives has led to the identification of SB-220453 20 with an in vivo pre-clinical CNS profile predictive of potential antimigraine activity.

Topics: Animals; Benzamides; Benzopyrans; Dose-Response Relationship, Drug; Methylcellulose; Mice; Migraine Disorders; Rats; Seizures; Sumatriptan; Temperature; Time Factors