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 C max and 3.0-fold higher AUC 0-∞ , while chito-cubosomes further enhanced bioavailability (5.0-fold) with prolonged MRT (2.2-fold) and delayed T max (2.8-fold). The results suggested that chito-cubosomes could be a promising drug carrier for enhancing oral absorption with sustained release behavior.
|Original language||English (US)|
|Number of pages||12|
|State||Published - 2019|
Bibliographical noteFunding Information:
This research was supported by National Natural Science Foundation of China (81703712, 81773675, 81873012), Natural Science Foundation of Jiangsu Province (BK20150703, BK20151438), “Double First-Class” University Project (CPU2018GY11, CPU2018GY27), Jiangsu Province Double Innovation Talent Program (2015), Top-notch Academic Programs Project of Jiangsu Higher Education Institutions (TAPP), Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD).
© 2019 The Royal Society of Chemistry.