PREPARATION AND IN VITRO EVALUATION OF MONTELUKAST SODIUM ORAL NANOEMULSION


Yasser Qasim Almajidi, Zainab H. Mahdi, Nidhal K. Maraie

Abstract


Objective: Oral nanoemulsion (NE) represent one of the newest technology to enhance drug intestinal 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, dispersability, 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.


Keywords


Montelukast sodium, nanoemulsion, oleic acid, ultrasonication

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