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OBJECTIVE： To prepare Paclitaxel（PTX）nanostructured lipid carriers （NLC） modified by small peptide alanine-glutamic acid-tyrosine-leucine-arginine （AEYLR）， and to evaluate its anti-tumor effect in vitro and in vivo. METHODS： NLC， PTX-NLC （P-NLC） and AEYLR modified P-NLC （A-P-NLC） were prepared by emulsion evaporation-low temperature solidification curing method. Its appearance， particle size， multi-dispersion index（PDI） and Zeta potential were characterized，encapsulation rate，drug loading and in vitro drug release were detected respectively. Using NCI-H1299 and S180 cells as objects， CCK-8 method was adopted to investigate inhibitory effects of free PTX， P-NLC and A-P-NLC （0.44-44.00 μg/mL， by PTX） to those cells. The half inhibition concentration （IC50） was calculated. Using S180 tumor-bearing mice as model animal， anti-tumor effects of free PTX， P-NLC and A-P-NLC （5 mg/kg， by PTX） were evaluated. RESULTS： P-NLC and A-P-NLC were round-like and dispersed evenly. The particle size， PDI and Zeta potential of A-P-NLC were （43.92±0.76） nm， 0.203±0.034 and （－19.77±1.16） mV， which were all increased to certain extent， compared with P-NLC. The encapsulation efficiency and drug loading of A-P-NLC were （95.71±0.68）％ and（1.97±0.25）％， which were both decreased to certain extent， compared with P-NLC. The cumulative release rate of A-P-NLC was（35.17±2.08）％ within 48 h， showing significant sustained-release effect compared with free PTX； the release of A-P-NLC was slower than P-NLC. Compared with free PTX and P-NLC， inhibitory rates of same concentration of A-P-NLC to NCI-H1299 cells and S180 cells were almost increased significantly， while IC50 values were all decreased significantly. There was no death in S180 tumor-bearing mice treated with A-P-NLC and the general condition was good； the volume of tumors was significantly reduced， the mass of tumors was significantly reduced， and the inhibition rate of tumors was significantly increased （P＜0.05 or P＜0.01）. CONCLUSIONS： A-P-NLC has significantly sustained-release effects； its inhibitory rate to NCI-H1299 cells and S180 cells in vitro， and its inhibitory effects on S180 solid tumor in mice are all better than free PTX and P-NLC， while the toxicity is decreased to certain extent.
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OBJECTIVE:To prepare Puerarin polymeric micelles and establish a method to determine its entrapment efficiency. METHODS:Puerarin polymeric micelles were prepared by film dispersion method. The polymeric micelles and free drug were sepa-rated by centrifugal-millipore filter filtration method. The entrapment efficiency of puerarin polymeric micelles was determined by HPLC. Diamonsil C18(2)column was used with 1% citric acid solution-methanol(65∶35)at the flow rate of 1 ml/min. The detec-tion wavelength was set at 250 nm,and column temperature was room temperature. RESULTS:The prepared polymeric micelles were spherical and spherical-like in shape with a mean particle size of 54.12 nm,polydispersity index of 0.122,Zeta potential of -13.60 mV;the linear range of puerarin was 2-10μg/ml(R2=0.999 4)with average recovery rate of 99.2%(RSD=0.9%,n=3). The re-covery rate of free drug was 95.3%(RSD=1.7%,n=3). The mean entrapment efficiency and drug-loading amount of puerarin were(35.5±2.12)% and(0.3±0.07)%,respectively(n=3). CONCLUSIONS:Film dispersion method is suitable for the prepara-tion of Puerarin polymeric micelles. Established method is convenient,accurate and reliable for the content and entrapment efficien-cy determination of Puerarin polymeric micelles.
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Objective To formulate the quality standard of Rukang Capsule. Method The TLC of Zhebeimu, Xuanshen, Ruxiang and Tiandong were done separately. The HPLC-ELSD was used to determine the content of Astragaloside in Mongolian Milkretch Root. Result There were the same spots between the controls and samples and an excellent linear relationship for 1.44～4.32 ?g to the content determination of Astragaloside. The average recovery can reach 100.3% with 0.5% of RSD. Conclusion This method is reliable and accurate to application, and can be used for the quality control of the preperation.
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Objective To determine whether the maternal serum interleukin-6(IL-6)and in- terleukin-8(IL-8)concentrations can be used in the antenatal diagnosis of intrauterine infection in premature rupture of membranes(PROM).Methods The level of maternal serum IL-6 and IL-8 were determined by a sensitive enzyme-linked immunosorbent assays in 50 normal late pregnant women,25 patients with PROM but without evidence of IAI and 49 patients with PROM and IAI. Results The maternal serum IL-6 and IL-8 concentrations in patients with PROM and IAI were 301.19?142.34/L and 312.32?149.56 ng/L,which were higher than that in patients with PROM but without IAI(133.22?55.26 ng/L and 125.35?61.30 ng/L)and the normal late pregnant wom- en were(126.59?57.12 ng/L and 112.69?56.02 ng/L),P
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To detect the soluble Fas (sFas) receptor level in sera from patients with myelodysplastic syndrome (MDS) and acute leukemia (AL), and investigate its clinical significance, the levels of sFas receptor in sera from 18 patients with MDS and 42 patients with AL were detected by using ELISA methods. The results suggested that the sFas receptor levels in sera from patients with MDS-RA were significantly lower than that from normal control (2.89?1.72 ng/ml vs 6.29?1.07 ng/ml, P