Supersaturated polymeric micelles for oral cyclosporine A delivery: The role of Soluplus-sodium dodecyl sulfate complex
Xia, DN; Yu, HZ; Tao, JS; Zeng, JR; Zhu, QL; Zhu, CL; Gan, Y; Gan, Y (reprint author), Chinese Acad Sci, Shanghai Inst Mat Med, 501 Haike Rd,Zhang Jiang Hi Tech Pk, Shanghai 201203, Peoples R China.
2016
发表期刊COLLOIDS AND SURFACES B-BIOINTERFACES
ISSN0927-7765
卷号141期号:-页码:301—310
文章类型期刊文献
摘要Our previous study demonstrated that the retention of drug in the hydrophobic core of Soluplus micelle greatly impeded drug absorption from gastrointestinal tract. Using supersaturated polymeric micelles can improve drug release, however, insufficient maintaining of supersaturation of drug is still unfavorable for drug absorption. Here, we report adding small amount of small molecule, sodium dodecyl sulfate (SDS), to Soluplus solution can form a Soluplus-SDS complex. This complex not only showed a higher solubilization capability for the model drug cyclosporine A (CsA), but also maintained a longer period of and higher supersaturation than was achieved with Soluplus alone. The Soluplus-SDS interactions were characterized by analyzing surface tension, small-angle X-ray scattering (SAXS), fluorescence spectra, and nuclear magnetic resonance spectroscopy. The results demonstrated that the formation of Soluplus-SDS complex via SDS adsorption on hydrophobic segments of Soluplus, which have more hydrophobic domain than that of Soluplus micelle, contributed significantly to the solubilization and stabilization of supersaturated CsA. Using this amphiphilic copolymer-small molecule surfactant system, the cellular uptake and rat in vivo absorption of CsA were more effectively achieved than pure Soluplus. The area under the plasma concentration-time curve (AUC) and the maximal plasma concentration (Cmax) achieved by CsA-loaded Soluplus-SDS complex were 1.58- and 1.8-times higher than the corresponding values for CsA-loaded pure Soluplus, respectively. This study highlighted the benefits of Soluplus-SDS complex for optimizing the solubilization and oral absorption of a drug with low aqueous solubility. (C) 2016 Elsevier B.V. All rights reserved.
关键词Solid Dispersions Administered Paclitaxel Cremophor-el Absorption Poly(Vinylpyrrolidone) Surfactants Dissolution Cellulose Pyrene
DOI10.1016/j.colsurfb.2016.01.047
收录类别SCI
语种英语
WOS记录号WOS:000374197700035
引用统计
被引频次:18[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.sinap.ac.cn/handle/331007/25852
专题中科院上海应用物理研究所2011-2018年
通讯作者Gan, Y (reprint author), Chinese Acad Sci, Shanghai Inst Mat Med, 501 Haike Rd,Zhang Jiang Hi Tech Pk, Shanghai 201203, Peoples R China.
推荐引用方式
GB/T 7714
Xia, DN,Yu, HZ,Tao, JS,et al. Supersaturated polymeric micelles for oral cyclosporine A delivery: The role of Soluplus-sodium dodecyl sulfate complex[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2016,141(-):301—310.
APA Xia, DN.,Yu, HZ.,Tao, JS.,Zeng, JR.,Zhu, QL.,...&Gan, Y .(2016).Supersaturated polymeric micelles for oral cyclosporine A delivery: The role of Soluplus-sodium dodecyl sulfate complex.COLLOIDS AND SURFACES B-BIOINTERFACES,141(-),301—310.
MLA Xia, DN,et al."Supersaturated polymeric micelles for oral cyclosporine A delivery: The role of Soluplus-sodium dodecyl sulfate complex".COLLOIDS AND SURFACES B-BIOINTERFACES 141.-(2016):301—310.
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