OBJECTIVETo prepare the quercetin self-emulsified formulation and evaluate its quality.

METHODThe quercetin self-emulsified formulation was optimized based on the quercetin solubility in different oils, and the self-microemulsified efficiency of various combinations of emulsifier and co-emulsifier evaluated using the pseudo-ternary phase diagram. The microemulsion of morphology, size and zeta potential were examined. The quercetin of solubility in self-emulsified system was tested and the formulation stability was investigated by accelerated experiment.

RESULTThe blank self-emulsified system was composed of ethyl oleate/Cremophor EUL/butanol with weight ratio of 10: 54: 36. After being dilutied with water, the morphology of microemulsion was homogeneous small spherical drops observed under the electro-microscopy. The particle size and the zeta potential were 16.3 +/- 4.6 nm and 2.1 +/- 0.8 mV, respectively. The solubility of quercetin in self-emulsifing system was (62.42 +/- 0.11) mg x mL(-1), increased 2 229 folds compared with that of in water. The quality of quercetin self-emulsified formulation was stable during the 3 months storage at 40 degrees C.

CONCLUSIONThe solubility of quercetin is significantly increased in self-emulsified system and the formulation is stable and easy to prepare.

Antioxidants ; administration & dosage ; chemistry ; Butanols ; chemistry ; Chromatography, High Pressure Liquid ; Drug Delivery Systems ; Drug Stability ; Emulsions ; Glycerol ; analogs & derivatives ; chemistry ; Oleic Acids ; chemistry ; Particle Size ; Quercetin ; administration & dosage ; chemistry ; Solubility ; Solvents ; Technology, Pharmaceutical ; methods

AIMTo investigate factors affecting the properties of antisense oligodeoxy nucleotides (ASON)-liposomes complex and their cellular uptake.

METHODSThree types of blank liposomes were prepared by reverse-phase evaporation vesicles, and the complex were obtained through physical absorption. The light microscope was used to observe morphology characteristics of the complex. Drug loading capacity was analyzed by agarose gel electrophoresis. The transfected cell percentage and means fluorescence intensity were determined by flow cytometric analysis using M3 myeloma cell as a model.

RESULTSThe neutral liposome showed no aggregation while the cationic liposomes appeared some different extent aggregation in different medium when associated antisense oligodeoxynucleotides. The drug loading capacity depended on the ratio of +/- and the cationic charge density on the lipid membrane. The two kinds of cationic liposomes appeared different principles of loading ASON. As far as cellular uptake, The neutral liposomes showed no improvement of cellular uptake of ASON. However, the cationic liposomes were shown to enhance the cellular uptake of ASON if the appropriate +/- charge ratio was used. The optimal cellular uptake was achieved when +/- charge ratio was at 0.5:1 and 1:1 for SA-I liposome and SA-II liposomes, respectively.

CONCLUSIONThe cationic liposomes improved the loading capacity and cell uptake of antisense oligodeoxynucleotides, which was determined by +/- charge ratio and charge density.

Amines ; metabolism ; Biological Transport ; Drug Carriers ; Drug Delivery Systems ; Humans ; Liposomes ; pharmacokinetics ; Multiple Myeloma ; Oligodeoxyribonucleotides, Antisense ; administration & dosage ; pharmacokinetics ; Random Allocation ; Tumor Cells, Cultured ; metabolism

Objective To quantify aqueous flare and cells in the eyes of healthy subjects and to evaluate the effect of age and sex on the blood aqueous barrier. Design Prospective case series. Participants Four hundred and forty-two eyes of 221 healthy sub- jects. Methods Aqueous flare and cells of 442 eyes were evaluated with FC-2000 laser flare cell meter (LFCM). Main Outcome Mea- sures Aqueous flare and cells. Results The mean flare values of all of eyes was 4.7?2.9 pc/ms, it was 3.1 pc/ms in the age group of less than 10 years, 3.8 pc/ms in the age group of 40-49 years and 11.0 pc/ms in the age group of 80 years or over. The mean flare val- ues in the age groups of 50 years or over were significantly higher than that in the age group of 40-49 years (P

AIMTo investigate the possibility of polymethacrylate nanoparticles (NP) for antisense oligodeoxynucleotides delivery system.

METHODSThe nanoparticles were prepared by evaporating ethenol solution containing Eudragit RL100 or RS100, and then mixtured with oligonucleotides. The morphology and size were investigated by a transmission electron microscope and Mastersizer particle characterization systems, and the cytotoxicity was evaluated by Trypan Blue staining and hemolysis test. The flow cytometer was used to determine the uptake of fluorescence-labelled oligodeoxynucleotides.

RESULTSThe morphology of nanoparticles showed spherical and orderly, the average diameter was about 127 nm, and almost the antisense oligodeoxynucleotides (ODN) were loaded when NP: ODN was 6.6. The uptake of ODN was significantly increased when loaded by nanoparticles, which well depended on the nanoparticles concentration. Meanwhile, slightly cytotoxicity was observed when high dose of nanoparticles was used.

CONCLUSIONThe polymethacrylate nanoparticles appeared to be a promising vehicle for gene delivery.

Acrylic Resins ; chemistry ; toxicity ; Animals ; Drug Carriers ; Drug Delivery Systems ; Hemolysis ; drug effects ; Nanotechnology ; Oligonucleotides, Antisense ; administration & dosage ; Particle Size ; Technology, Pharmaceutical ; methods

AIMTo survey the uptake behavior and subcellular distribution of antisense oligodeoxynucleotide polymethacrylate submicroparticles (AS-ODN-SMP) and infer its mechanism in MGC cell lines.

METHODSMGC cells were incubated at certain concentration of AS-ODN-SMP or AS-ODN for 8 h at 4 degrees C or 37 degrees C. Then the fluorescence oligodeoxynucleotide- labeled cells were counted by flow cytometer and the intracellular fluorescence intensity was determined after incubated with chloroquine for 2 h.

RESULTSCellular uptake of oligodeoxynucleotides was significantly increased following application of AS-ODN-SMP and total intracellular fluorescence intensity was enhanced by 683 folds with the vehicle concentration of 20 microg x mL(-1). AS-ODN-SMP entranced to cells profoundly with temperature-dependent manner. Rare cells took on fluorescence when incubated at 4 degrees C, while 37 degrees C they were significantly increased. But the intracellular fluorescence intensity appeared same level in present or absent of chloroquine.

CONCLUSIONWith the help of polyacrylate submicroparticles, oligonucleotides efficiently entranced the cells via endocytosis and could successfully escape the degradation in lysosome.

Animals ; Cell Line ; Drug Carriers ; Drug Delivery Systems ; Endocytosis ; drug effects ; Giant Cells ; cytology ; Lysosomes ; metabolism ; Nanoparticles ; Oligodeoxyribonucleotides, Antisense ; administration & dosage ; pharmacokinetics ; Particle Size ; Polymethacrylic Acids ; chemistry ; pharmacology ; Temperature

Adult ; China ; epidemiology ; Humans ; Male ; Meningitis, Meningococcal ; epidemiology ; microbiology ; Neisseria meningitidis, Serogroup W-135 ; genetics ; isolation & purification

The chemical constituents from the fruiting bodies of Lyophyllum decastes (Fr.) Singer were studied in this paper. Thirteen compounds were isolated and purified by column chromatographies on silica gel and Sephadex LH-20. Their structures were identified by MS and NMR data analysis as adenosine (1), 2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxyheneicosanoylamino]-8-octadecene-1, 3, 4-triol (2), (2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxypentacosanoylamino]-8-octadecene-1, 3, 4-triol (3), nicotinic acid (4), (4E, 8E) -2-N-2-hydroxytetracosanoyl-1-O-beta-D-glycopyranosyl-9-methyl-4, 8-sphingadienine (5), D-mannitol (6), ergosteryl-3-O-beta-D-glucopyranoside (7), tuberoside (8), (2R, 3S, 4S, 8E)-2-[(2'R)-2-hydroxybehenoylamino]-8-octadecene-1, 3, 4-triol (9),(2R, 3S, 4S, 8E)-2-[(2'R) -2-hydroxytricosanoylamino] -8-octadecene-1, 3, 4-triol (10), (22E, 24R)-ergosta-7, 22-dien-3beta, 5alpha, 6beta-triol (11), (22E, 24R)-ergosta-5, 7, 22-trien-3beta-ol (12), and 5alpha, 8alpha-epidiory-(22E, 24R)-ergosta-6, 22-dien-3beta-ol (13), respectively. All the above compounds are first obtained from the mushroom and compounds 2-10 are reported to be obtained from the Lyophyllum for the first time.
Agaricales ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Fruit ; chemistry

Objective To analyse the causes of perinatal death and explore the preventive measures to reduce the perinatal mortality.Methods The cases with perinatal death in this hospital from January 2005 to December 2006 were reviewed to analyse the causes of death by categorization and sum-up.Results There were 166 cases with perinatal death and the mortality rate was 27.08‰,including 126 cases with fatal death,which accounted for 75.90%.In the analysis of dead causes,the first one was birth defects,which suffered 69 cases,41.57% of all,and mostly were with fetus edema syndrome.The cord factors had been elevated to the second cause,which suffered 51 cases,30.72% of all.Conclusion Improving the consciousness of gestational monitoring and self-care,strengthening the prenatal diagnosis and genetic counseling,controlling the perinatal birth defects,monitoring mother and fetus by poly-parameter and stopping the pregnancy in time can reduce perinatal death effectively.

Objective: To investigate the changes of gene expression in CD34+ hematopoietic stem and progenitor cells (HSPCs) under different growth environments. Methods: Umbilical cord blood mononuclear cells (UCB MNCs) were cultured in static and stirred systems. After 7 days of culture, CD34+ cells were isolated and total RNA was extracted. Gene expression patterns of CD34+ cells from fresh, static and stirred cultures were compared using differential display (DD). Results: 30 gene fragments displayed differential expression levels based on the conditions of DD. One of differentially expressed genes was identified as RAN, which is a member of oncogene RAS family. This gene may be associated with proliferation of hematopoietic cells. Conclusion: Different growth environments induced differential gene expression patterns of CD34+ HSPCs. These differentially expressed genes would give new insights into optimizing in vitro environments for expanding hematopoietic cells.