Phospholipid complex is one of the most successful approaches for enhancing oral\nbioavailability of poorly absorbed plant constituents. But the sticky property of phospholipids\nresults in an unsatisfactory dissolution of drugs. In this study, a matrix dispersion of baicalein\nbased on phospholipid complex (BaPC-MD) was first prepared by a discontinuous solvent\nevaporation method, in which polyvinylpyrrolidone-K30 (PVP-K30) was employed for improving\nthe dispersibility of baicalein phospholipid complex (BaPC) and increasing dissolution of\nbaicalein. The combination ratio of baicalein and phospholipids in BaPC-MD was 99.39% and\nbaicalein was still in a complete complex state with phospholipid in BaPC-MD. Differential\nscanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM) and\nFourier Transform Infrared (FTIR) analyzes demonstrated that baicalein was fully transformed\nto an amorphous state in BaPC-MD and phospholipid complex formed. The water-solubility and\nn-octanol solubility of baicalein in BaPC-MD significantly increased compared with those of\npure baicalein. Compared with baicalein and BaPC, the cumulative dissolution of BaPC-MD at\n120 min increased 2.77- and 1.23-fold, respectively. In vitro permeability study in Caco-2 cells\nindicated that the permeability of BaPC-MD was remarkably higher than those of baicalein and\nBaPC. Pharmacokinetic study showed that the average Cmax of BaPC-MD was significantly\nincreased compared to baicalein and BaPC. AUC0ââ?¬â??14 h of BaPC-MD was 5.01- and 1.91-fold of\nbaicalein and BaPC, respectively. The novel BaPC-MD significantly enhanced the oral\nbioavailability of baicalein by improving the dissolution and permeability of baicalein without\ndestroying the complexation state of baicalein and phospholipids. The current drug delivery\nsystem provided an optimal strategy to significantly enhance oral bioavailability for poorly\nwater-soluble drugs.
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