International Journal of Biological Macromolecules 2015-01-01

Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant.

Eun-Sol Ha, Jinsu Ok, Jongmin Noh, Hee-Young Jeong, Gwang-Ho Choo, Young-Suk Jung, In-Hwan Baek, Jeong-Soo Kim, Wonkyung Cho, Sung-Joo Hwang, Min-Soo Kim

Index: Int. J. Biol. Macromol. 72 , 1473-8, (2014)

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Abstract

This study was undertaken to improve the solubility and dissolution of a poorly water-soluble drug, celecoxib, by surface modification with a hydrophilic polymer and a surfactant by using a spray-drying technique. Based on the preliminary solubility tests, hydroxypropylmethyl cellulose (HPMC) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were selected as the polymer and the surfactant, respectively. A novel surface-modified celecoxib microparticle was successfully fabricated using a spray-drying process with water, HPMC, and TPGS, and without the use of an organic solvent. The physicochemical properties of the surface-modified celecoxib microparticle were characterized using scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), a particle size analyzer, and contact angle determination. The formulation with drug/HPMC/TPGS at the weight ratio of 1:0.5:1.5 was determined to be the most effective composition in the preparation of the surface-modified celecoxib microparticle, based on the results of wettability, solubility, and dissolution studies. We found that the surface modification of microparticles with HPMC and TPGS can be an effective formulation strategy for new dosage forms of poorly water-soluble active pharmaceutical ingredients (APIs) to provide higher solubility and dissolution.Copyright © 2014 Elsevier B.V. All rights reserved.