Development of Sildenafil Microemulsion for Rapid Rapid-Onset Nasal Spray

摘要

An oleic acid acid-based microemulsion system withCremophor EL or Tween series as surfactants, and short short-chain alcohol as cosolvents was developed for rapid rapid-onsetintranasal delivery of sildenafil. Phase behavior andsolubilization capacity of the microemulsion system werecharacterized and in vivo nasal absorption of sildenafilfrom microemulsion formulations was investi investigated ingated rabbits. A single isotropic region, which is considered as amicroemulsion, was found in the pseudo pseudo-ternary phasediagrams developed at various surfactants: cosolventsratios. With the higher weight percentage of surfactant,the region area of mic microemulsion in the phase diagramroemulsion decreasing, the viscosity of microemulsion increased.Sildenafil, a water water-insoluble drug, displayed a highsolubility of 12 124 mg/ml in a microemulsion consisting of40% oleic acid, 10% H H2O, and 50% Tween 80 O, 80: propanol: (at 1:4 weight ratio ratio). Nasal absorption of sildenafil from). This microemulsion was found to be fairly rapid. At 10 mgdose, the maximum drug plasma concentration wasarrived at 26.7 ± 5.8 min, and the onset of action wasabout 8.5 min. These results suggest that th themicroemulsion system composed of oleic acid, Tween 80,propanol and water may be a useful approach for therapid rapid-onset delivery of sildenafil with the erectiledysfunction.