title: Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant.
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.
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Eun-Sol
authors.initials: ES
authors.lastname: Ha
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Jinsu
authors.initials: J
authors.lastname: Ok
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Jongmin
authors.initials: J
authors.lastname: Noh
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Hee-Young
authors.initials: HY
authors.lastname: Jeong
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Gwang-Ho
authors.initials: GH
authors.lastname: Choo
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea.
authors.forename: Young-Suk
authors.initials: YS
authors.lastname: Jung
authors.affiliation: College of Pharmacy, Kyungsung University, Daeyeon-dong, Nam-gu, Busan 608-736, Republic of Korea.
authors.forename: In-Hwan
authors.initials: IH
authors.lastname: Baek
authors.affiliation: College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Republic of Korea.
authors.forename: Jeong-Soo
authors.initials: JS
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Republic of Korea; Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea.
authors.forename: Wonkyung
authors.initials: W
authors.lastname: Cho
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea; College of Pharmacy, Yonsei University, 162-1 Songdo-dong, Yeonsu-gu, Incheon 406-840, Republic of Korea.
authors.forename: Sung-Joo
authors.initials: SJ
authors.lastname: Hwang
authors.affiliation: College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan 609-735, Republic of Korea. Electronic address: minsookim@pusan.ac.kr.
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
mesh_terms: D000068579:Celecoxib; D005079:Excipients / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D065347:Hypromellose Derivatives / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*; D012995:Solubility; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology*; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*; D014810:Vitamin E / Q000031:analogs & derivatives* / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D005079:Excipients; D011720:Pyrazoles; D013449:Sulfonamides; D013501:Surface-Active Agents; D014810:Vitamin E; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; D000068579:Celecoxib; C014225:tocophersolan
keywords: Celecoxib; Dissolution; Surface modification