title: Enhanced dissolution of celecoxib by supersaturating self-emulsifying drug delivery system (S-SEDDS) formulation.
abstract: A supersaturating self-emulsifying drug delivery system (S-SEDDS) was prepared and evaluated for enhanced dissolution of celecoxib (CXB), a poorly water-soluble drug. The selected CXB-dissolved SEDDS formulation consisting 10 % Capryol 90 (oil), 45 % Tween 20 (surfactant), and 45 % Tetraglycol (cosurfactant) had the characteristics of small droplet size and great solubility as 208 nm and 556.7 mg/mL in average, respectively. CXB dissolution from SEDDS in simulated gastric fluid was increased to about 20 % for the initial period of 5 min, but decreased to a half level as time elapsed. Thus, precipitation inhibitors were screened to stabilize the supersaturation. The stabilizing effect of Soluplus, an amphiphilic copolymer, was concentration-dependent, revealing the greatest dissolution of approximately 90 % level with delayed drug crystallization by the addition of the copolymer. CXB dissolution from S-SEDDS was pH-independent. We concluded that S-SEDDS formulation would be very useful in the future for developing oral delivery product of poorly water-soluble drugs.
authors: Drug Delivery Research Laboratory, College of Pharmacy, Chung-Ang University, 221 Heuksuk-dong, Dongjak-gu, Seoul 156-756, South Korea.
authors: Woo Heon
authors: WH
authors: Song
authors: Jong Hyeok
authors: JH
authors: Park
authors: Dong Woo
authors: DW
authors: Yeom
authors: Byeong Kil
authors: BK
authors: Ahn
authors: Kyung Min
authors: KM
authors: Lee
authors: Sang Gon
authors: SG
authors: Lee
authors: Hye Seung
authors: HS
authors: Woo
authors: Young Wook
authors: YW
authors: Choi
mesh_terms: D002210:Caprylates / Q000737:chemistry; D000068579:Celecoxib; D002626:Chemistry, Pharmaceutical; D052246:Cyclooxygenase 2 Inhibitors / Q000008:administration & dosage* / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D008823:Micelles; D010316:Particle Size; D044367:Phase Transition; D011720:Pyrazoles / Q000008:administration & dosage* / Q000737:chemistry*; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage* / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D002210:Caprylates; D052246:Cyclooxygenase 2 Inhibitors; D004337:Drug Carriers; D004655:Emulsions; D008823:Micelles; D011720:Pyrazoles; D013449:Sulfonamides; D013501:Surface-Active Agents; D000068579:Celecoxib