Author(s):

Cheng Zeng, Wen Jiang, Xin-chun Wang, Mei-e Tan, Jian-guo Xing

Abstract: To prepare Composite Phospholipid Liposome (CPL) of Total Flavonoids Extract from Dracocephalum moldavica (TFDM), determine its physicochemical properties, investigate its in-vitro release and increase the bioavailability of TFDMCPL. The CPL was prepared by ammonium sulfate transmembrane gradients. The CPL and TFDM were separated by Sephadex-G50 chromatography. The concentration of TFDM in the CPL were detected by HPLC, then the entrapment efficiency (EE) was evaluated. And the shape, particle size, zeta potential, drug release in vitro were investigated, differential scanning calorimetry (DSC) techniques was employed to investigate molecular interaction in TFDMCPL and study the transcellular transportation and cytotoxicity of TFDMCPL using Caco-2 cell model. The EE of TFDM was 84.17±2.2%, mean size of CPL was 136.2±3.7 nm, polymey disperse index (PDI) was 0.158±0.015 and zeta potential was -19.8±1.2 mV. TFDMCPL were found to enhance the release of drugs more effectively than TFDM based on the in vitro model and CPL were found to enhance the permeability of TFDM more effectively than the TFDM alone based on the in vitro model of the epithelial barrier. The ammonium sulfate transmembrane gradient is suitable for preparing TFDMCPL. This HPLC method was accurate and sensitive, and can be applied to the determination of TFDMCPL. And TFDMCPL have potential to be used to improve the bioavailability of poorly soluble drugs after oral administration.

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