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Objective To research the optimal preparation technology of salinomycin micelle.Methods DSPE-PEG2000 was selected as the carrier.Salinomycin was selected as the model drug.The film dispersion method, the ethanol injection method and the dialysis method were used to prepare salinomycin micelles respectively.The comprehensive evaluation indexes included entrapment rate and drug-loading rate, release capacity and vitro cytotoxicity test in order to select the most suitable preparation technology of salinomycin micelle .Results The film dispersion method is the most suitable preparation technology of salinomycin micelle in the three methods.Its average grain diameter was (14 ±2.3) nm, entrapment rate was (82 ± 2.6)%, drug-loading rate was (6.3 ±2.1)%, IC50 to HepG2 tumor cells was 16.10 ±3.71.Conclusion The film dispersion method of salinomycin micelles has the advantages with the smallest size, the highest entrapment rate and the largest drug-loading rate, which has the function to kill tunmor cells and release slowly.
ABSTRACT
OBJECTIVE: To prepare armillarisin A-loaded nanostructured lipid carriers (AML-NLC) for intravenous injection and investigate its release characteristics in vitro and its pharmacokinetics in rats. METHODS: Armillarisin A-loaded nanostructured lipid carriers for intravenous injection were prepared by emulsification-ultrasonication and lyophilization. The shapes and sizes of the lipid nanoparticles and the drug-loading capability were evaluated. Entrapment efficiency was determined by microdialysis method. The in vitro drug release behavior was investigated by dialysis method. The pharmacokinetics in rats were compared with those of armillarisin A injection. RESULTS: The mean particle size, entrapment efficiency and drug-loading capability were 111 nm, (75.7 ± 1.34)% and (0.04 ± 0.01)%, respectively. The in vitro cumulative release rate in pH 5.6 phosphate buffer reached above 90% in 48 h. The in vitro drug release behavior was fitted well by Weibull equation. The elimination half lives of AML injection and AML-NLC after iv injection in rats were 59.7 and 115.2 min, respectively. And the absolute bioavailability of AMLS-NLC was 151.1%. CONCLUSION: Armillarisin A lipid nanoparticles are prepared by emulsification-ultrasonication and lyophilization, which show high entrapment rate and even distribution. The lipid nanoparticles show sustained release in vitro compared with ordinary injection. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVE:To establish an RP-HPLC method for the content determination of glycyrrhizic acid in gly-cyrrhizin liposome.METHODS:The separation was performed on Shim-pack VP-ODS column with methanol-buffer phosphate(pH=2.6,68∶32)as the mobile phase,the detection wavelength was254nm and the flow rate was1ml/min.RE-SULTS:Glycyrrhizic acid was well-separated with peaks of the adjuvants and the solvent.The linear range for glycyrrhizic acid was1～100?g/ml(r=0.9999,n=5).The average recovery was97.56%(RSD=1.03%).CONCLUSION:This method is accurate and sensitive,and suitable for the content determination of glycyrrhizic acid in glycyrrhizin liposome.