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Cubosomes with surface cross-linked chitosan exhibit sustained release and bioavailability enhancement for vinpocetine

Authors :
Yuan Gao
Changquan Calvin Sun
Shuai Qian
Chengran Liu
Yuanfeng Wei
Yaxiang Gong
Jianjun Zhang
Meng Fu
Zheng Yazhen
Liang Xu
Source :
RSC Advances. 9:6287-6298
Publication Year :
2019
Publisher :
Royal Society of Chemistry (RSC), 2019.

Abstract

The present study aims to develop cubosomes with surface cross-linked chitosan for sustained drug delivery and enhanced oral bioavailability of vinpocetine (VPT). GMO based liquid cubosomes with VPT loading were prepared by the high pressure homogenization method. In order to enhance the anti-digestion effect, chitosan was cross-linked on cubosomes by the Schiff reaction, followed by solidification via spray drying. The obtained spray-dried cubosomes (chito-cubosomes) are spherical microspheres with nano-sized holes on the surface. After reconstitution, the particle size and zeta potential of chito-cubosomes were determined to be ∼250 nm and +35.9 mV, respectively. In comparison to unmodified liquid cubosomes, chito-cubosomes exhibited a significant anti-digestion effect with a typical sustained release profile. In comparison to a VPT suspension, liquid cubosomes showed a 2.5-fold higher Cmax and 3.0-fold higher AUC0–∞, while chito-cubosomes further enhanced bioavailability (5.0-fold) with prolonged MRT (2.2-fold) and delayed Tmax (2.8-fold). The results suggested that chito-cubosomes could be a promising drug carrier for enhancing oral absorption with sustained release behavior.

Details

ISSN :
20462069
Volume :
9
Database :
OpenAIRE
Journal :
RSC Advances
Accession number :
edsair.doi.dedup.....d950760aab36a239933c7c7b53a00784
Full Text :
https://doi.org/10.1039/c8ra10302j