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Ibuprofen (IBU) is one of the most commonly used nonsteroidal anti-inflammatory drugs with high permeability and low solubility. The aims of this research is to improve the solubility and dissolution of the IBU by reducing particle size using ultrasonic spray drying method and utilizing watersoluble polymer (polyvinyl alcohol (PVA)) and surfactant (sodium lauryl sulphate (SLS)) for particles formulation. The results showed that increasing amount of PVA, smaller particle size of as-prepared IBU-PVA-SLS was obtained, 6.3-fold smaller than untreated IBU. The in vitro drug release study for simulated gastric fluid without enzymes (0.1 N HCl or Buffer pH 1.2) shows the dissolution of prepared IBU-PVA-SLS significantly increase 2.4-fold higher than untreated IBU for dissolution time of 30 minutes. While the solubility of the IBU-PVA-SLS was increased 4.7-fold compare to untreated IBU. In general, IBU possessing relatively high dissolution in intestinal fluid. In contrast, the finding of recent investigation on dissolution of IBU-PVA-SLS is significantly increase in gastric fluid, either due to smaller particles size or PVA-SLS. Thus, despite the PVA and SLS determine the particles formation during polymerization yielding smaller particle size, they also responsible for effective drug delivery system. It was concluded that PVA and SLS in ultrasonic spray drying technique for IBU preparation successfully reduces the particle size and effectively enhances the solubility and dissolution rate of poorly water-soluble IBU in 0.1 N HCl. [ABSTRACT FROM AUTHOR]