Ursolic acid nanoparticles for oral delivery prepared by emulsion solvent evaporation method: characterization, in vitro evaluation of radical scavenging activity and bioavailability.

摘要: With the purpose of improving water solubility and oral bioavailability, ursolic acid nanoparticles (UANs) were prepared by emulsion solvent evaporation method, nanosuspension was freeze-dried into powder. The optimal conditions for preparing screened out using single-factor experiment. Take advantage conditions, UA nanoemulsion had mean particle size (MPS) 69.7 ± 15.6 nm polydispersity index value (PI) 0.005. MPS gained at 100.2 12.1 (PI = 0.005), after organic removed rotary evaporator. Finally, UANs possessing an 157.5 28.0 0.005) zeta potential 20.33 1.67 mV obtained freeze-dried. investigated SEM, XRD, DSC, TGA further explored their equilibrium solubility, dissolution rate, residue analysis, cellular antioxidant activity bioavailability. All results above showed that in amorphous state. result test figured 13.48 times simulated gastric fluid (SGF), 11.79 intestinal (SIF) 23.99 deionized than raw UA. Accordingly, rate SGF SIF apparent enhancement. bioavailability increased 2.68 improved toward cells compared with UA, EC50 reduced 37.5 residual contents trichloromethane ethanol separated up to mustard ICH limit class III II solvents. indicated possesses a application on enhancement