Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe

Title
Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe
Author(s)
김종오레마나라시드[레마나라시드]김동욱[김동욱]아비드[아비드]오메르[오메르]박종혁[박종혁]용철순오유경[오유경]윤유석[윤유석]최한곤[최한곤]파카르[파카르]
Keywords
IN-VIVO EVALUATION; MULTIDRUG-RESISTANCE PHENOTYPE; CREMOPHOR-EL; PHYSICOCHEMICAL CHARACTERIZATION; INTESTINAL-ABSORPTION; ORAL BIOAVAILABILITY; DOSAGE FORMS; SMEDDS; STABILITY; OPTIMIZATION
Issue Date
201509
Publisher
DOVE MEDICAL PRESS LTD
Citation
INTERNATIONAL JOURNAL OF NANOMEDICINE, v.10
Abstract
Background: The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimibe-loaded solid self-nanoemulsifying drug delivery system (SNEDDS), surface modified solid dispersion (SMSD), and solvent evaporated solid dispersion (SESD) to identify the best drug delivery system with the highest oral bioavailability. Methods: For the liquid SNEDDS formulation, Capryol 90, Cremophor EL, and Tween 80 were selected as the oil, surfactant, and cosurfactant, respectively. The nanoemulsion-forming region was sketched using a pseudoternary phase diagram on the basis of reduced emulsion size. The optimized liquid SNEDDS was converted to solid SNEDDS by spray drying with silicon dioxide. Furthermore, SMSDs were prepared using the spray drying technique with various amounts of hydroxypropylcellulose and Tween 80, optimized on the basis of their drug solubility. The SESD formulation was prepared with the same composition of optimized SMSD. The aqueous solubility, dissolution, physicochemical properties, and pharmacokinetics of all of the formulations were investigated and compared with the drug powder. Results: The drug existed in the crystalline form in SMSD, but was changed into an amorphous form in SNEDDS and SESD, giving particle sizes of approximately 24, 6, and 11 mu m, respectively. All of these formulations significantly improved the aqueous solubility and dissolution in the order of solid SNEDDS >= SESD > SMSD, and showed a total higher plasma concentration than did the drug powder. Moreover, SESD gave a higher area under the drug concentration time curve from zero to infinity than did SNEDDS and SMSD, even if they were not significantly different, suggesting more improved oral bioavailability. Conclusion: Among the various formulations tested in this study, the SESD system would be strongly recommended as a drug delivery system for the oral administration of ezetimibe with poor water solubility.
URI
http://hdl.handle.net/YU.REPOSITORY/31011http://dx.doi.org/10.2147/IJN.S91216
ISSN
1178-2013
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약학대학 > 약학부 > Articles
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