Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus-PVPVA complex.
10.1016/j.apsb.2018.09.004
- Author:
Chunliu ZHU
1
;
Shuang GONG
2
;
Jinsong DING
2
;
Miaorong YU
3
;
Ejaj AHMAD
3
;
Yi FENG
1
;
Yong GAN
3
Author Information
1. Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
2. Xiangya School of Pharmaceutical Science, Central South University, Changsha 410000, China.
3. Shanghai Institute of Materia Medica, Chinese Academy of Science, Shanghai 201203, China.
- Publication Type:Journal Article
- Keywords:
Complex;
Oral bioavailability;
PVPVA;
Silybin;
Soluplus;
Supersaturated drug delivery system
- From:
Acta Pharmaceutica Sinica B
2019;9(1):107-117
- CountryChina
- Language:English
-
Abstract:
Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system (SDDS). In this study, we reported a complex system of Soluplus-Copovidone (Soluplus-PVPVA) loaded with the model drug silybin (SLB) that could not only maintain the stability of a supersaturated solution but also effectively promote oral absorption. The antiprecipitation effect of the polymers on SLB was observed using the solvent-shift method. In addition, the effects of the polymers on absorption were detected by cellular uptake and transport experiments. The mechanisms by which the Soluplus-PVPVA complex promotes oral absorption were explored by dynamic light scattering, transmission electron microscopy, fluorescence spectra and isothermal titration calorimetry analyses. Furthermore, a pharmacokinetic study in rats was used to demonstrate the advantages of the Soluplus-PVPVA complex. The results showed that Soluplus and PVPVA spontaneously formed complexes in aqueous solution the adsorption of PVPVA on the hydrophilic-hydrophobic interface of the Soluplus micelle, and the Soluplus-PVPVA complex significantly increased the absorption of SLB. In conclusion, the Soluplus-PVPVA complex is a potential SDDS for improving the bioavailability of hydrophobic drugs.
