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Enhanced dissolution of celecoxib by supersaturating self-emulsifying drug delivery system (S-SEDDS) formulation

Author:
Song, Woo Heon, Park, Jong Hyeok, Yeom, Dong Woo, Ahn, Byeong Kil, Lee, Kyung Min, Lee, Sang Gon, Woo, Hye Seung, Choi, Young Wook
Source:
Archives of pharmacal research 2013 v.36 no.1 pp. 69-78
ISSN:
0253-6269
Subject:
composite polymers, crystallization, droplet size, drug delivery systems, drugs, gastric juice, oils, polysorbates, solubility, surfactants
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.
Agid:
112852