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.

Evaluation of Blatta orientalis (Q) nasal gel formulation in milk aspiration induced eosinophilia.

BACKGROUND: The purpose of the present study was to develop intranasal delivery systems of the homeopathic anti-asthmatic remedy Blatta orientalis mother tincture (Q) using thermoreversible polymer Pluronic F127 (PF127) and mucoadhesive polymer Carbopol 934P (C934P). METHODS: Formulations were modulated so as to have a gelation temperature below 34 degrees C to ensure gelation at physiological temperature after intranasal administration. Its gelation temperature, mucoadhesive strength, viscosity and gel strength were studied. B. orientalis (Q) nasal gel was tested with recurrent milk aspiration to determine whether it produces changes in eosinophilia in a murine model of asthma. RESULT: The gelation temperatures of the formulations and mucoadhesive strength, determined using sheep nasal mucosal membrane, increased by the addition of increasing concentrations of Carbopol. The results of milk aspiration induced eosinophilia, B. orientalis (Q) nasal gel significantly (P < 0.001), decreased eosinophil cell count as compared with toxicant by using in absolute eosinophilia count method. Finally, histopathological examination did not detect any damage during in vivo studies. CONCLUSION: The PF127 gel formulation of B. orientalis (Q) with in situ gelling and mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption.

Formulation and evaluation of in situ gelling system of dimenhydrinate for nasal administration.

Nasal drug delivery has a variety of advantages. Drugs can be rapidly absorbed through the nasal mucosa, giving rapid onset of action, and avoiding presystemic metabolism. In present study; the nasal mucoadhesive in situ gels of anti-emetic drug Dimenhydrinate were formulated using Gellan gum and Carbopol 934P. The in situ gels so prepared were characterized for gelation, viscosity, gel strength, mucoadhesion, drug content, drug diffusion, ex vivo permeation and histopathological studies. The optimized formulation passing from above tests was further subjected to accelerated stability study. It retained the good stability over the period of 90 days. From the overall performance this in situ gel seems to be an effective delivery system for the nasal route.