ABSTRACT
OBJECTIVE： To prepare Syringopicroside solid lipid nanoparticles （SYR-SLN）， and optimize the formula and characterize SYR-SLN. METHODS： SYR-SLN were prepared by emulsion evaporation method. Using entrapment efficiency as index， based on single factor， orthogonal design was adopted to optimize the mass ratio of lecithin-monoglyceride， volume ratio of organ phase to water phase， poloxamer 188 （F68） concentration and drug dosage. The optimal formula technology was established to investigate entrapment efficiency， drug-loading amount， morphology， particle size， Zeta potential， stability， etc. RESULTS： The mass ratio of lecithin-monoglyceride was 3 ∶ 1； the volume ratio of organic phase to water phase was 1 ∶ 2； the concentration of F68 was 0.4％； drug dosage was 10 mg. The optimal formula included that monoglyceride 80 mg， lecithin 240 mg， 0.4％ F68， syringopicroside 10 mg， absolute ethyl alcohol 5 mL， distilled water 10 mL， emulsification temperature at 65℃ and stirring at 600 r/min. Encapsulation efficiency of SYR-SLN was （42.35±0.60）％ （n＝3）； drug-loading amount was （5.33±0.03）％ （n＝3）； SYR-SLN had a spherical morphology and was evenly distributed. The average particle size was （180.30±5.31） nm with Zeta potential of （－41.9±0.8） mV， and the SYR-SLN could maintain stable for 15 days at 4℃. CONCLUSIONS： SYR-SLN is prepared successfully， and the technology is simple with high encapsulation efficiency.
ABSTRACT
Objective To investigate the uptake mechanism of HepG2.2.15 cells to the nanoparticles co-loaded with syringopicroside and hydroxytyrosol (SH-NPs). Methods The nanoparticles were prepared by using a nanoprecipitation method with mPEG-PLGA as nano-carrier co-loaded with syringopicroside and hydroxytyrosol. The uptake mechanism of HepG2.2.15 cells to SH-NPs was studied by fluorescence microscopy and flow cytometry using fluoresceineisothiocyanate (FITC) as a fluorescent marker. Results With colchicine as the inhibitor, the incubation time ranged from 0.5 to 24 h, the percentage of positive cells increased from 1.9% to 56.4%; When the drug concentration was 125, 250 μg/mL and 500 μg/mL, the positive cell percentages were 4.9%, 3.4% and 3.9%. With chloroquine as the inhibitor; the incubation time ranged from 0.5 to 24 h, the percentage of positive cells increased from 7.4% to 55.4%; When the drug concentration was 125, 250 and 500 μg/mL, the percentage of positive cells was 19.5%, 22.5% and 27.6%. Conclusion Colchicine and chloroquine have an inhibitory effect on HepG2.2.15 cells uptake, and the uptake of SH-NPs in HepG2.2.15 cells was positively correlated with drug concentration and incubation time. It can be concluded that the uptake mechanism of HepG2.2.15 cells to SH-NPs was nonspecific adsorption endocytosis.
ABSTRACT
Objective: To study the chemical components from the rhizomes of Cyperus rotundus. Methods: The compounds were isolated and purified by chromatographic techniques, and their structures were elucidated by spectral methods. Results: A new isoflavonoid, 5, 7, 4'-trihydroxy-2'-methoxy-3'-prenylisoflavone (1), along with nine phenolic compounds, 6-O-p-hydroxybenzoyl- 6-epi-aucubin (2), 6-O-p-hydroxybenzoyl-6-epi-monomelittoside (3), verproside (4), syringopicroside B (5), syringopicroside C (6), oleuropeinic acid (7), oleuroside (8), 10-hydroxyoleuropein (9), and senburiside I (10), were obtained from the rhizomes of C. rotundus. Conclusion: Compound 1 is a new isoflavone, named cyperotundone A, and compounds 2-10 are isolated from this plant for the first time.