ABSTRACT
AIM To prepare the liposomes loaded with celastrol,tanshinone Ⅱ A and tanshinone Ⅱ A sodium sulfonate and to evaluate the effects of preparation technologies and entrapment materials on the encapsulation efficiencies.METHODS The liposomes for three constituents were prepared by film dispersion method and reverse phase evaporation method,respectively.50％ Lecithin high potency,80％ egg yolk lecithin,92％ lecithin high potency and complex phospholipid (5 ∶ 1 for ratio of dipalmitoyl phosphatidylcholine to 50％ lecithin high potency) were served as entrapment materials.The encapsulation efficiencies were thus calculated based on the measured ean sizes and polydispersity of the liposomes.RESULTS Celastrol and tanshinone Ⅱ A sodium sulfonate liposomes accomplished by reverse phase evaporation method got the highest encapsulation efficiency when entrapped with 80％ egg yolk lecithin and 92％ lecithin high potency,respectively,which were higher than those prepared by film dispersion method.And celastrol liposomes exhibited an even superior performance than tanshinone Ⅱ A sodium sulfonate liposomes.Tanshinone Ⅱ A lipisome prepared by film dispersion method and then entrapped with 50％ lecithin high potency obtained its the highest value of encapsulation efficiency,which was much lower than those of another two liposomes.CONCLUSION Reverse phase evaporation method is appropriate for hydrophobic celastrol with multiple hydrogen bonds and hydrophilic sodium tanshinone Ⅱ A without hydrogen bonds to prepare their liposomes,while film dispersion method is applicable to hydrophobic tanshinone Ⅱ A without hydrogen bonds.
ABSTRACT
Objective: To synthesize butyryl galactose ester (But-Gal) and prepare butyryl galactose ester-modified coix component microemulsions (But-Gal-CMEs) and to evaluate its physicochemical properties and anticancer activity in vitro. Methods: But-Gal was synthesized by enzyme-catalyzed reaction and the structure of the product was confirmed by 1H-NMR and FT-IR. The CMEs and But-Gal-CMEs were prepared by aqueous titration method using coix seed oil, Cremophor RH40, PEG400, But-Gal, and coixan solution as oil phase, surfactant, cosurfactant, target ligand, and aqueous phase, respectively. The average particle size, polydispersity index (PDI), and Zeta potential were detected by dynamic light scattering (DLS). The cytotoxicity of CMEs and But-Gal-CMEs aganist HepG2 cells was determined by MTT assay. The cellular uptake of CMEs and But-Gal-CMEs was detected by fluorescence microscopy. Results: The structure of But-Gal was confirmed by 1H-NMR and FT-IR. The But-Gal-CMEs displayed the spherical surface with mean droplet size of (57.68 ± 6.65) nm, PDI of 0.070 ± 0.006, and Zeta potential of (-2.95 ± 0.23) mV, respectively. MTT experiments showed that the half of HepG2 cell proliferation inhibition concentration (IC50) of But-Gal-CMEs and CMEs was 62.55 and 71.23 μg/mL. The HepG2 cell uptake results suggested that the fluorescence intensity of But-Gal-CMEs group was higher than that of CMEs group. Conclusion: The But-Gal-CMEs presents small particle size, good roundness, and good stability. In addition, But-Gal could increase the uptake rate of CMEs in HepG2 cells and enhance the inhibition of HepG2 cell proliferation.