Formulation, Optimization and Characterization of Ibuprofen Loaded Microemulsion System Using D-Optimal Mixture Design

Abstract

Objective: The purpose of this study was to develop, optimize and characterize a stable microemulsion, with an improvement of the solubility of a poorly aqueous soluble drug, ibuprofen.
 Methods: Various oils (oleic acid, cottonseed oil, olive oil, argan oil, and labrafac® WL 1349), surfactants (tween® 80, tween® 40, tween® 20) and co-surfactants including polyethylene glycol 400, ethanol, 1-butanol, and propylene glycol were selected after solubility studies. Then, pseudo-ternary phase diagrams with surfactant/co-surfactant ratio of 1:2, 1:1, 2:1 and 3:1 were constructed and a D-optimal mixture design method was used to optimize the ibuprofen loaded microemulsion. The optimized microemulsion was evaluated for several characteristics including globule size, zeta potential, pH, conductivity, refractive index and stability studies.
 Results: Optimized microemulsion obtained was composed of oleic acid (6.88% w/w), tween® 80/1-butanol (3:1, 63.11% w/w) and water (30.00% w/w). The results obtained showed an average globule size of 117.5 nm, a zeta potential of-6.47 mV and a transmittance of 96.95±0.77%. The optimized formulation showed an improvement in the solubility of ibuprofen with unchanged characteristics for one month.
 Conclusion: The use of pseudo-ternary phase diagrams and mathematical modeling allows to obtain an optimal microemulsion with perfect stability for 1 mo and a better solubilization capacity of ibuprofen.

Physicochemical and microbiological evaluation of ibuprofen suspension produced using Detarium microcarpum as suspending agent

“…12,13 Ibuprofen, a non-steroidal anti-inflammatory drug (NSAID) is utilized in the treatment of pain caused by headaches, toothaches, back pain, rheumatoid arthritis, osteoarthritis and slight injuries. It is used to relieve muscle spasm, and in reducing fever and any other nonspecific inflammation 14,15 . It is a phenyl propionic acid derivative ((RS)-2-(4-(2methylpropyl) phenyl) -propionic acid) and one of the best tolerated NSAIDs.…”

“…It is a phenyl propionic acid derivative ((RS)-2-(4-(2methylpropyl) phenyl) -propionic acid) and one of the best tolerated NSAIDs. 14,15 It is a non-selective inhibitor of cyclooxygenase-1 (COX-1) and Cyclooxygenase-2 (COX-2). Ibuprofen is almost insoluble in water and this makes it a good candidate for suspension formulation.…”

Foray into Concepts of Design and Evaluation of Microemulsions as a Modern Approach for Topical Applications in Acne Pathology

“…The selected API in microemulsion formulation is protected against hydrolytic and oxidative processes, being incorporated as encapsulated particles in oil or water fine droplets; MEs have a superior stability with improvement in half life. [177,179] 7.…”