Preparation and <Emphasis Type="Italic">in vitro</Emphasis> evaluation of povidone-sodium cholate-phospholipid mixed micelles for the solubilization of poorly soluble drugs |
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Authors: | Yuan Zhu Jiangnan Yu Shanshan Tong Li Wang Min Peng Xia Cao Ximing Xu |
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Institution: | (1) Bioavailability Control Laboratory, College of Pharmacy, Kangwon National University, 1 University Road, Hyoja-Dong, Chuncheon, 200-701, Republic of Korea; |
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Abstract: | Mixed micelles made of polyvinylpyrrolidone (PVP), sodium cholate, and phospholipids were prepared to improve the solubility
of poorly water-soluble drugs. Sylibin, a drug used in treating liver diseases, was incorporated into the mixed micelles.
The formulation of sylibin containing PVP-sodium cholate-phospholipid mixed micelles with an optimized composition (PVP/sodium
cholate/phospholipid/silybin = 3:3:4:1∼2 by weight) was obtained based on the study of pseudoternary phase diagrams. The critical
micelle concentration was used to evaluate the micellar stability towards dilution. The results showed that addition of PVP
to sodium-cholate-phospholipid mixed micelles increased stability. The solubility of sylibin in PVP-sodium cholate-phospholipid
mixed micelles was higher than that in pure water or in sodium cholate-phospholipid mixed micelles. In a stability study,
we found that PVP-sodium cholate-phospholipid mixed micelles showed good stability. After 3 months storage at 40°C, just 2.6%
sylibin was lost with only minor changes of the particle size when compared to a reference formulation containing sodium cholate
and phospholipid mixed micelles. In addition, the developed formulation significantly improved in vitro drug release. The time required to release 50% sylibin (t50%) from sodium cholate and phospholipid mixed micelles was 326
h, while the t50% from PVP-sodium cholate-phospholipid mixed micelles was only 51.1 h. Our results suggest that these mixed
micelles might have significant potential application to the biomedical field. |
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