Study On Liposome Capillary Electrophoretic For Hydrophobicity Of Organic Compounds

Because of the similar to the biomembrane both in the structure and constitute, liposome is used as the model of the biomembrane. In the paper, liposome capillary electrophoresis(LCE) was used to determine the hydrophobic parameter of organic compounds, which could more better reflect the partition to the biomembrane. The main research and results are as below:â‘ The LCE method to determine the hydrophobic parameter of compounds was established. The tl was obtained by non-linearity fitting with logPow values from literature and measured migration time (tm) of a series of organic compounds, a calibration curve for estimating logP of compounds was thus obtained. The logP values of six benzenes measured by this method were close to those determined by shake-flask method and by MEEKC method, and the average error between values from the two methods were 0.35 and 0.38 logarithm units respectively, which was aroused by the different system. But the average error between values from iteration and non- iteration was only 0.07 logarithm units. The hydrophobic parameters of four neutral and four charged pharmaceuticals were determined by the LCE method. The logP values of four neutral and charged pharmaceuticals measured by the LCE method were close to those determined by shake-flask method, and the average error between values from two methods were 0.28 and 0.84 logarithm units. The great average error was evaluated from the determined model.â‘¡LCE was used as a model for the in vitro evaluation of the oil-solute and the degree of membrane penetration. The hydrophobic parameters of nine compounds were determined by the LCE method. Compared with the relativity of logk in LCE and logPm, logPow and logPm, it was told that the relativity of logk in LCE and logPm was larger. It also proved that as the biomembrane model, liposome is more similar than the octanol/water system. The LCE method has the potential to be an in vitro screening model at the early stage of the drug discovery process.In the paper, The LCE method for determination of hydrophobic parameter of compounds was established. The LCE method is simply and fast, which would provide a new method for determination of hydrophobic parameter of compounds, especially for drugs.