Effects of Bile Salt-Phosphatidylcholine-Mixed Micelles on the Solubility of Hydrophobic Drugs

摘要

Objective: To research the effects of bile Salt-Phosphatidylcholine-Mixed Micelles (BS/PC-MM) on the solubility of hydrophobic drugs and relevant factors. Methods: sodium deoxycholate/soya phosphatidylcholine, SDC/SPC-MM was prepared by dissolving with agitation. The particle size distribution and zeta potential were measured by the dynamic light scattering (DLS) and the electrophoretic light scattering (ELS). Ginsenosides 20 (S)-Rg3, Rh2, Astragaloside Ⅳ, 20 (S)-protopanaxadiol and Furanodiene were dissolved in SDC/SPC-MM with different proportions of SDC and SPC. The solubility was quantified by HPLC. Results: SDC increased the solubility of SPC hydroxyl groups and prepared MM satisfied the requirements of MM systems. The solubility of Ginsenosides 20 (S)-Rg3, Rh2, Astragaloside Ⅳ increased with the percentage of SDC whereas the solubility of hydrophobic drugs, 20 (S)-protopanaxadiol, 20 (S)-protopanaxadiol and Furanodiene was increased with SPC. Conclusions: The hydrophobic groups within SPC enhanced the affinity to hydrophobic drugs whereas hydrophilic groups within ginsenosides inhibit the effects of SPC on its solubility. The effects of SDC/SPC-MM on drug solubility depend on the proportion of SDC and SPC. The solubility of hydrophobic drugs also depends on chemical structure, molecular weight and polarity of the drugs.