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Development of cyclosporin A-loaded hyaluronic microsphere with enhanced oral bioavailability

Title
Development of cyclosporin A-loaded hyaluronic microsphere with enhanced oral bioavailability
Author
최한곤
Keywords
bioavailability; cyclosporin A; sodium hyaluronate; sodium lauryl sulfate; microsphere; spray drying
Issue Date
2007-12
Publisher
ELSEVIER SCIENCE BV
Citation
INTERNATIONAL JOURNAL OF PHARMACEUTICS, v. 345, No. 1-2, Page. 134-141
Abstract
To develop a hyaluronic microsphere with the improved oral bioavailability of poorly water-soluble cyclosporin A (CsA), the microspheres were prepared with varying ratios of sodium hyaluronate (HA)/sodium lauryl sulfate (SLS)/CsA using a spray-drying technique. The effects of HA and SLS on the dissolution and solubility of CsA in microspheres were investigated. The CsA-microsphere prepared with HA/SLS/CsA at the ratio of 4/2/1 gave the highest solubility and dissolution rate of CsA among those formulae tested. As solubility and dissolution rate of CsA were increased about 17- and 2-fold compared to CsA powder, respectively, this CsA-microsphere was selected as an optimal formula for oral delivery in rats. The CsA-microsphere and Sandimmun neoral sol((R)) gave significantly higher blood levels compared with CsA powder alone. Moreover, the AUC, T-max and C-max values of CsA in CsA-microsphere were not significantly different from those in Sandimmun neoral sol((R)) in rats, indicating that CsA-microsphere was bioequivalent to the commercial product in rats. Our results demonstrated that the CsA-microsphere prepared with HA and SLS, with improved bioavailability of CsA, might have been useful to deliver a poorly water-soluble CsA. (c) 2007 Elsevier B.V. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S037851730700748Xhttp://repository.hanyang.ac.kr/handle/20.500.11754/107162
ISSN
0378-5173; 1873-3476
DOI
10.1016/j.ijpharm.2007.08.050
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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