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Comparison of three different types of cilostazol-loaded solid dispersion: Physicochemical characterization and pharmacokinetics in rats

Title
Comparison of three different types of cilostazol-loaded solid dispersion: Physicochemical characterization and pharmacokinetics in rats
Author
최한곤
Keywords
Cilostazol; Solvent-evaporated solid dispersion; Solvent-wetted solid dispersion; Surface-attached solid dispersion; Solubility; Crystallinity; Oral bioavailability; IN-VIVO EVALUATION; SPRAY-DRYING TECHNIQUE; ORAL BIOAVAILABILITY; GELATIN MICROCAPSULE; ENHANCED SOLUBILITY; AQUEOUS SOLUBILITY; DRUG-DELIVERY; BEAGLE DOGS; TWEEN 80; FENOFIBRATE
Issue Date
2017-03
Publisher
ELSEVIER SCIENCE BV
Citation
COLLOIDS AND SURFACES B-BIOINTERFACES, v. 154, Page. 89-95
Abstract
The aim of this research was to compare three different types of cilostazol-loaded solid dispersion system including solvent-evaporated, solvent-wetted and surface-attached solid dispersion. The effect of polymers and surfactants on the aqueous solubility of cilostazol was investigated, leading to the selection of polyvinylpyrrolidone (PVP) and sodium lauryl sulphate (SLS). Employing a spray-drying technique, numerous surface-attached, solvent-evaporated and solvent-wetted solid dispersions were prepared with various amounts PVP and SLS using water, 90% ethanol and acetone, respectively. Their physicochemical properties, solubility, dissolution and oral bioavailability in rats were assessed, compared to the drug powder. Among each solid dispersion system tested, the surface-attached, solvent-evaporated and solvent-wetted solid dispersions composed of cilostazol, PVP and SLS at weight ratios of 3.0 : 0.75 :1.5, 3.0 :3.0 : 1.5 and 3.0 : 3.0 : 1.5, respectively, provided the highest drug solubility and dissolution. The solvent-evaporated solid dispersion gave homogeneous and very small spherical particles, in which the drug was changed to an amorphous state. In the solvent-wetted solid dispersion, the amorphous drug was attached to the polymer surface. Conversely, in the surface-attached solid dispersion, the carriers were adhered onto the surface of the unchanged crystalline drug. The solubility, dissolution and oral bioavailability were significantly increased in the order of solvent-evaporated ˃ solvent-wetted ˃ surface attached ˃ drug powder. Thus, the type of solid dispersion considerably affected the physicochemical properties, aqueous solubility and oral bioavailability. Furthermore, the cilostazol-loaded solvent evaporated solid dispersion with the highest oral bioavailability would be actively recommended as a practical oral pharmaceutical product. (C) 2017 Elsevier B.V. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0927776517301352http://repository.hanyang.ac.kr/handle/20.500.11754/71818
ISSN
0927-7765; 1873-4367
DOI
10.1016/j.colsurfb.2017.03.017
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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