Thermoreversible-mucoadhesive Gel for nasal delivery of sumatriptan

Abstract

The purpose of the present study was to develop intranasal delivery systems of sumatriptan using thermoreversible polymer Pluronic F127 (PF127) and mucoadhesive polymer Carbopol 934P (C934P). Formulations were modulated so as to have gelation temperature below 34°C to ensure gelation at physiological temperature after intranasal administration. Gelation temperature was determined by physical appearance as well as by rheological measurement. The gelation temperatures of the formulations decreased by addition of increasing concentrations of Carbopol (ie, from 29°C for 18% PF127 to 23.9°C for 18% PF127, 0.5% Carbopol). The mucoadhesive force in terms of detachment stress, determined using sheep nasal mucosal membrane, increased with increasing concentration of Carbopol. The results of in vitro drug permeation studies across sheep nasal mucosa indicate that effective permeation coefficient could be significantly increased by using in situ gelling formulation with Carbopol concentration 0.3% or greater. Finally, histopathological examination did not detect any damage during in vitro permeation studies. In conclusion, the PF127 gel formulation of sumatriptan with in situ gelling and mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption.

Development ofin situgel for nasal delivery: design, optimization,in vitroandin vivoevaluation

“…Phosphate buffer pH 6.4 and isopropyl alcohol were used as negative and positive controls, respectively (Majithiya et al, 2006). Histological studies were carried out on sheep nasal mucosa that had been used for ex vivo permeation study which was treated with 1 ml optimized in situ gel for 5 h. After treatment, tissue were cut and stained with eosin.…”

“…Moreover, the transport of sumatriptan across the blood-brain barrier is very poor. After 15 minutes, sumatriptan solution is swallowed and it enters the gastrointestinal tract where remaining dose is absorbed, which may get increased by intranasal delivery (Ryan et al, 1997;Majithiya et al, 2006). An intranasal-microemulsion drug delivery system to accomplish rapid delivery of sumatriptan to the brain in acute attacks of migraine has been reported (Vyas et al, 2005).…”

“…An intranasal-microemulsion drug delivery system to accomplish rapid delivery of sumatriptan to the brain in acute attacks of migraine has been reported (Vyas et al, 2005). The PF127 gel formulation of sumatriptan with in situ gelling and mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption (Majithiya et al, 2006).…”

Synthesis and characterization of a cysteine xyloglucan conjugate as mucoadhesive polymer

“…The probe was then moved upwards by adding weight in pan which is present on other side of balance. The mucoadhesive force, expressed as the detachment stress in dyne/cm 2 , was determined from the minimal weights that detached the tissues from the surface of each formulation using the following equation (Majithiya et al, 2006). Detachment Stress (dyne/cm 2 ) = m* g/ A where m is the weight added to the balance in grams; g is the acceleration due to gravity taken as 980 cm/s 2 ; and A the area of tissue exposed.…”

Nasal-nanotechnology: revolution for efficient therapeutics delivery

“…These systems are appears as liquids in storage conditions but converted to gels at the site of application. This conversion is triggered by the pH (Nakamura et al, 1999), temperature (Majithiya et al, 2006;Mahajan et al, 2012), presence of any other ionic or biological component, etc.…”