Open AccessThe preparation and investigation of spinosin–phospholipid complex self‐microemulsifying drug delivery system based on the absorption characteristics of spinosin
Author(s) -
Song Panpan,
Lai Changjiangsheng,
Xie Junbo,
Zhang Yanqing
Publication year - 2019
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.13076
Subject(s) - drug , phospholipid , drug delivery , pharmacology , chemistry , chromatography , absorption (acoustics) , medicine , materials science , organic chemistry , biochemistry , composite material , membrane
Objectives The aim of this research was to investigate the intestinal absorption characteristics and mechanisms of spinosin ( SPI ), and a new dosage form was prepared to increase the intestinal absorption of SPI . Methods In this study, the intestinal absorption characteristics and mechanisms of SPI were first investigated using in situ absorption model and Caco‐2 monolayer model. Subsequently, the phospholipid complex ( PLC ) loaded with SPI was prepared followed by a self‐microemulsifying drug delivery system ( SMEDDS ) technique for developing a more efficient formulation. Key findings The results showed that the absorption rate constant (0.02 h −1 ) and absorption percentage (10%) of SPI were small. Paracellular and active transport pathways mainly mediated the intestinal absorption of SPI . Moreover, SPI ‐ PLC ‐ SMEDDS showed a nanoscale particle size and excellent dispersibility in vitro . The cellular uptake and transportation properties of SPI ‐ PLC ‐ SMEDDS in the Caco‐2 cell model were improved significantly. Besides, a statistically dramatically higher oral bioavailability (almost fivefold) was observed following the oral administration of SPI ‐ PLC ‐ SMEDDS than free SPI on the basis of pharmacokinetic experiment results. Furthermore, the SPI ‐ PLC ‐ SMEDDS exhibited certain immunization. Conclusions SPI ‐ PLC ‐ SMEDDS could be a promising oral drug delivery system to improve the absorption of SPI .