Abstract
Objective: Oral nanoemulsion (NE) represent one of the newest technology to enhance intestinal drug permeability, bioavailability and facilitate swallowing of the oral dosage form.Methods: In this study, montelukast sodium (MS) nanoemulsions (NEs) were formulated by ultra-sonication using different surfactants (tween 20, tween 60 and tween 80) in different surfactant: co-surfactant (ethanol) ratios (Smix). The prepared NEs were evaluated for different parameters including droplet size (DS) using zetasizer as a function of ultra-sonication time, dispersibility, phase separation, conductivity, percent transmittance, optical transparency, in vitro release in addition to morphology using transmission electron microscopic (TEM).Results: The results revealed that F3 was the optimum formula having an average DS 32.95±2.8 nm after 5 min ultra-sonication assured by zetasizer and TEM, furthermore, a clear to bluish NE was formed after aqueous dilution with high conductivity (59.2±1.76 μs/cm) which indicated the formation of O/W NE. In addition, an optically clear NE was formed with (88.6±2.1) % transmittance with no sedimentation, creaming or separation after centrifugation signifying the formation of a stable NE. Finally, F3 showed faster dissolution rate (92.45%±1.66) after 30 min compared to other formulas.Conclusion: The net result of this study is the formulation of a stable oral NE containing MS which presents new easily swallowed dosage form that may enhance drug permeability as well as it may reduce drug metabolism leading to improving bioavailability for asthmatic patients.
Highlights
IntroductionNanoemulsions (NEs) are thermodynamically stable dispersion of oil and water with deformable droplets in the range of (10–200 nanometre “nm”) which have specific physicochemical properties such as low viscosity, transparency, optical isotropy and does not have the tendency to coalesce due to the presence of a stabilizing surfactant: co-surfactant mixture
Oral administration is the most preferred route for administration of pharmaceuticals, it is restricted by swallowing difficulty of the solid dosage form in addition to dissolution, absorption and bioavailability problems [1, 2].For many years, numerous technologies were developed to produce swallowed dosage forms and to enhance its oral bioavailability, from which oral nanoemulsion (NE) was one of the most promising investments [3, 4].Nanoemulsions (NEs) are thermodynamically stable dispersion of oil and water with deformable droplets in the range of (10–200 nanometre “nm”) which have specific physicochemical properties such as low viscosity, transparency, optical isotropy and does not have the tendency to coalesce due to the presence of a stabilizing surfactant: co-surfactant mixture
Their small elastic droplets give them higher stability because the diffusion rate is higher than the sedimentation or creaming rate induced by the gravity force
Summary
Nanoemulsions (NEs) are thermodynamically stable dispersion of oil and water with deformable droplets in the range of (10–200 nanometre “nm”) which have specific physicochemical properties such as low viscosity, transparency, optical isotropy and does not have the tendency to coalesce due to the presence of a stabilizing surfactant: co-surfactant mixture. Their small elastic droplets give them higher stability because the diffusion rate is higher than the sedimentation or creaming rate induced by the gravity force. Montelukast is marketed as the sodium salt in the form of tablets and inhalers, no liquid dosage form is available because of the stability problem of this salt in the aqueous media [9, 10]
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