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The aim of the study was to improve the oral absorption of the compound 25-OCH 3 -PPD with poor hydrophilicity and lipophilicity. 25-OCH 3 -PPD-phospholipid complex was prepared by solvent evaporation, then characterized by differential scanning calorimetry, scanning electron microscopy, and infrared absorption spectroscopy. The aqueous solubility and oil-water partition coefficient were compared with the free compound. A nanoemulsion loaded with 25-OCH 3 -PPD-phospholipid complex was developed by dissolving the complex in water in the presence of hydrophilic surfactant under sonication. After oral administration of the nanoemulsion and the suspension of 25-OCH 3 -PPD in rats, the concentrations of 25-OCH 3 -PPD in plasma were determined by high-performance liquid chromatography-tandem mass spectrometry method. The results showed that the solubility of the complex in water and n-octanol was enhanced. The oil-water partition coefficient improved 1.7 times. Peak plasma concentration and area under the curve (0-24 h) of the nanoemulsion of 25-OCH 3 -PPD-phospholipid complex were higher than that of free compound by 3.9- and 3.5-folds.

drug design, development and therapy

Improved oral bioavailability of 20(R)-25-methoxyl-dammarane-3&amp;beta;, 12&amp;beta;, 20-triol using nanoemulsion based on phospholipid complex: design, characterization, and in vivo pharmacokinetics in rats