The objectives of this study are to prepare resveratrol loaded mixed micelles composed of poloxamer 403 and poloxamer 407, and optimize the formulation in order to achieve higher drug solubility and sustained drug release. Firstly, a thin-film hydration method was utilized to prepare the micelles. By using drug-loading, encapsulation yield and particle size of the micelles as criteria, influence of three variables, namely poloxamer 407 mass fraction, amount of water and feeding of resveratrol, on the quality of the micelles was optimized with a central composite design method. Steady fluorescence measurement was carried out to evaluate the critical micelle concentration of the carriers. Micelle stability upon dilution with simulated gastric fluid and simulated intestinal fluid was investigated. The in vitro release of resveratrol from the mixed micelles was monitored by dialysis method. It was observed that the particle size of the optimized micelle formulation was 24 nm, with drug-loading 11.78%, and encapsulation yield 82.51%. The mixed micelles increased the solubility of resveratrol for about 197 times. Moreover, the mixed micelles had a low critical micelle concentration of 0.05 mg · mL(-1) in water and no apparent changes in particle size and drug content were observed upon micelles dilution, indicating improved kinetic stability. Resveratrol was released from the micelles in a controlled manner for over 20 h, and the release process can be well described by Higuchi equation. Therefore, resveratrol-loaded poloxamer 403/407 mixed micelles could improve the solubility of resveratrol significantly and sustained drug release behavior can be achieved.
Drug Carriers ; chemistry ; Fluorescence ; Kinetics ; Micelles ; Particle Size ; Poloxamer ; chemistry ; Solubility ; Stilbenes ; chemistry ; Water

Objective To investigate the value of the application of the fresh first morning midstream urine in cytological study of bladder cancer patients. Methods The results of the fresh first and second morning midstream urine cytological studies for 52 bladder cancer patients were analyzed.Continual three urine samples and single urine sample were treated as study objects respectively. The positive rates in different tumor stages and grades were evaluated. Results The positive rate of overall 52 patients was 78. 8 % (41/52) in fresh first morning midstream urine and 80. 8% ( 42 / 52) in the fresh second morning midstream urine. While in 156 single urine samples, the positive percentages were 56.4%(88/156) and 60. 9% (95/156). The positive rates of the fresh first and second morning midstream urine were 69.7% (23/33) and 72.7% (24/33) respectively in grade 1- 2 patients, and 44.4 % (44/99) and 48. 5 % (48/99) in 99 single urine samples. The positive rates of 42 non-muscle invasive bladder cancer patients were 73. 8% (31/42) and 76.2% (32/42) in the fresh first and second morning midstream urine, while in 126 single urine samples, the positive rates were 54.8% (69/126)and 57.1% (72/126). There were no significant differences between positive rate of the fresh first and second morning midstream urine in diagnosis of bladder cancer, low grade bladder cancer and nonmuscle invasive bladder cancer. Conclusion The fresh first morning midstream urine can be used for urine cytological study in the diagnosis of bladder cancer, even in the diagnosis of low stage and low grade bladder cancer.

Objective To evaluate the use of gated SPECT in patients with hypertrophic obstructive cardiomyopathy (HOCM) and the effects of percutaneous transluminal septal myocardial ablation (PTSMA) on myocardial perfusion.Methods 99 Tcm-methoxyisobutylisonitrile (MIBI) and 18F-fluorodeoxyglucose (FDG) images were performed in 31 HOCM patients before PFSMA and in 15 patients 3-7 d after PTSMA.The images in different left ventricular segments were analysed by using scores.Results In 99Tcm-MIBI images, uptake decreased at the septal regions in 12 HOCM patients (80.0%, 12/15) after PTSMA, 18F-FDG images also showed decreased uptake at the septal regions in 5 HOCM patients (33.3%, 5/15) after PTSMA.Conclusion 99Tcm-MIBI images might be an important method to evaluate PTSMA results, and 18 F-FDG images showed important value as reference.

OBJECTIVETo study the effects of citalopram on the expression of proliferating cell nuclear antigen (PCNA) and proto-oncogene protein (C-fos) and cell apoptosis in frontal cortical neurons of rat after stress.

METHODSTwenty four healthy male SD rats were randomly divided into three groups (n = 8): control group, stress group (treated with saline, ig) , experimental group (treated with Citalopram 4 mg/kg x d for 28 days, ig). Rats were forced to swim to establish chronic stress model. The protein expression levels of PCNA and C-fos were tested by immunohistochemistry assay. TUNEL assay was used to test cell apoptosis. Nikon image analysis software was used to determine the number of positive cells in each index.

RESULTSCompared with the control group, the stress group showed a smaller amount of PCNA-positive cells, a larger number of C-fos positive cells, and the volume of positive cells was significantly reduced. Compared with the stress group, the PCNA positive cells were increased significantly, the C-fos positive cells and TUNEL positive cells were decreased significantly, nuclear condensation phenomenon in frontal cortical neurons and the staining was significantly lighter in experimental group (P < 0.05).

CONCLUSIONCitalopram significantly antagonize PCNA, C-fos protein expression and cell apoptosis of rat prefrontal cortical neurons caused by chronic stress, which might be the one of mechanisms of citalopram for prevention and treatment of psychosis caused by chronic stress.

Animals ; Apoptosis ; drug effects ; Citalopram ; pharmacology ; Frontal Lobe ; cytology ; Immunohistochemistry ; Male ; Neurons ; cytology ; drug effects ; Proliferating Cell Nuclear Antigen ; metabolism ; Proto-Oncogene Proteins c-fos ; metabolism ; Rats ; Rats, Sprague-Dawley ; Stress, Physiological

OBJECTIVETo prepare an ultrasound microbubble contrast agent using PLLA-PEG-PLLA copolymer as the shell material, and test their acoustic characteristics in vitro.

METHODSPLLA-PEG-PLLA tri-block co-polymers were synthesized by ring-opening polymerization. Microbubbles were prepared by using double emulsion technique. Light microscope and scanning electron microscope were applied to observe the morphology of the microbubbles. Their size distribution was analyzed using MASTERSIZER 2000. The acoustic characteristics of microbubbles were tested by using color Doppler Ultrasonography.

RESULTSMicrobubbles were well dispersed in water. Contrast enhancement was stronger and longer lasting at low mechanical index.

CONCLUSIONThe polymer-encapsulated microbubbles prepared by using double emulsion technique with PLLA-PEG-PLLA as the shell material can be used as an ultrasound contrast agent.

Contrast Media ; chemistry ; Drug Compounding ; Lactates ; chemistry ; Microbubbles ; Polyesters ; chemistry ; Polyethylene Glycols ; chemistry ; Ultrasonography, Doppler, Color ; methods

Objective To study the expression patterns of Th1 and Th2 cytokine genes in childhood acute idiopathic thrombocytopenic purpura(ITP) and its clinical value.Methods Peripheral blood samples from 30 patients with acute ITP before and after treatment (ITP group) and those from 20 normal healthy subjects (healthy control group) were collected (healthy control group),and reverse transcriptases polymerase chain reaction was performed to determine the mRNA expressions of Th1 and Th2 cytokine genes before and after treatment,which were compared with those of the health controls.Results The positive rate of expression levels of Th1 cytokine genes in samples from ITP patients (3.3％,3.3％) were significantly lower than those from healthy control group (all P ＜ 0.05) and increased to normal level after treatment(16.7％,23.3％).In contrast,Th2 cytokine genes (IL-4,IL-6,IL-10)in the samples from the ITP patients(33.3％,43.3％,40.0％) were significantly higher than those from the healthy control group (all P ＜0.05) and decreased after treatment(10.0％,23.3％,20.0％).Conclusions Such data indicate that ITP is a Th2 cell predominant autoimmune disease,and the abnormal immunity due to Th1/Th2 shift is significant in the pathogenesis of ITP.

Betulinic acid is a naturally occurring pentacyclic triterpenoid, which has antiretroviral, antimalarial, and anti-inflammatory properties. The purpose of this study is to investigate the HBV DNA replication inhibition in the mouse model with betulinic acid. Hydrodynamic injection method via the tail vein with the Paywl. 3 plasmid was used to establish the animal mode (n = 15), and the mice were randomly divided into the PBS control group (n = 5), Betulinic acid treatment group (n = 5) and lamivudine control group (n = 5). The day after successful modeling , the mice would have taken Betulinic acid (100 mg x kg(-1)), lamivudine (50 mg x kg(-1)), PBS drugs orally, once daily for 7 days, blood samples were acquired from the orbital venous blood at 3, 5, 7 days after the administering, HBsAg and HBeAg in serum concentration were measured by ELISA and the mice were sacrificed after 7 days, HBV DNA southern detections were used with part of mice livers. The results showed that betulinic acid significantly inhibited the expression of HbsAg in the mice model at the fifth day compared with the control group, and there was no significant differences between the effects of lamivudine and the PBS control group; both the betulinic acid and lamivudine groups had no significant inhibition for the HBeAg expression; the HBV DNA expressions of the liver tissue from the betulinic acid and lamivudine groups were inhibited compared with the control group. Taken together, these results reveal betulinic acid can inhibit the HBsAg expression and replication of the liver HBV DNA in the mouse model.
Acute Disease ; Animals ; Antiviral Agents ; pharmacology ; DNA Replication ; drug effects ; DNA, Viral ; biosynthesis ; Hepatitis B ; blood ; virology ; Hepatitis B Surface Antigens ; blood ; Hepatitis B virus ; drug effects ; genetics ; immunology ; physiology ; Male ; Mice ; Plasmids ; genetics ; Triterpenes ; pharmacology ; Virus Replication ; drug effects

OBJECTIVETo evaluate the diagnosis and management of adrenal myelolipoma.

METHODSThe clinical data of 26 cases were analyzed retrospectively and the selected articles were reviewed. There were no specific clinical symptom and endocrine abnormality, except increasing catecholamine in 2 cases. All cases but two were diagnosed by B-model ultrasound scanning (B-US), CT or magnetic resonance imaging (MRI).

RESULTSTwenty-six cases were surgically treated, the diameter of the tumor was 5 - 10 cm, simple tumor resection was performed in 16 cases, and complete adrenal resection was performed in 10 cases. All the operated cases were proved by pathologists. The duration of follow-up was from 6 - 28 months after surgery. No recurrence was observed.

CONCLUSIONSThe diagnosis of adrenal myelolipoma could be established based on B-US, CT or MRI. The tumors whose diameter is larger than 5 cm in size should be removed.

Adrenal Gland Neoplasms ; diagnosis ; surgery ; Adrenalectomy ; Adult ; Female ; Follow-Up Studies ; Humans ; Magnetic Resonance Imaging ; Male ; Middle Aged ; Myelolipoma ; diagnosis ; surgery ; Retrospective Studies ; Tomography, X-Ray Computed

Objective To investigate the relevant factors of coronary artery disease (CAD) in young people under 40 years of age.
Methods The study population was 292 young patients accepting coronary angiography in Fuwai Hospital from July to December 2006, including 272 men and 20 women, with the mean age being 36.7±3.7 years. The diagnosis of CAD was made in the cases presenting ≥50%stenosis in coronary lumen in coronary angiography. Based on the diagnosis, 217 patients (204 men, 13 women) were assigned to CAD group, and 75 (68 men, 7 women) to non-CAD group. Clinical data and metabolic characteristics of the patients were collected and analyzed using t-test,χ2 test, and multinomial logistic regression with SPSS 8.0 software.
Results Most study subjects were current smokers (209/292, 71.6%), and more than half had body mass index (BMI)>24 kg/m2 (230/292, 78.8%) and usually took high-fat diet (162/292, 55.5%). The proportion of heavy smokers (smoking history ≥10 years and ≥20 cigarettes per day) were significantly higher in the CAD group than in the non-CAD group [20.7%(45/217) vs. 9.3%(7/75), P=0.015)]. Heavy smoking [odds ratio (OR), 1.89;95%confidence interval (CI), 1.74-2.05], hypertension (OR, 1.56;95%CI, 1.48-1.65), alcohol (OR, 1.37;95%CI, 1.30-1.46), type 2 diabetes mellitus (OR, 1.37;95%CI, 1.25-1.50), high-fat diet (OR, 1.35;95% CI, 1.28-1.43), and BMI>24 kg/m2 (OR, 1.09;95% CI, 1.03-1.17) were factors related to CAD in the young patients (all P<0.05). Total cholesterol (4.56±1.46 mmol/L vs. 4.09±1.00 mmol/L), low-density lipoprotein cholesterol (2.38±1.11 mmol/L vs. 2.14±0.63 mmol/L), lipoprotein a (134.97±109.70 mg/L vs. 101.58±58.39 mg/L), uric acid (359.89±100.09 μmol/L vs. 336.75±94.36μmol/L), erythrocyte sedimentation rate (9.98±12.19 mm/hour vs. 4.89±4.92 mm/hour), high-sensitivity C-reactive protein (3.42±4.39 mg/L vs. 2.80±3.77 mg/L) and Big endothelin-1 (1.41±1.50 fmol/mL vs. 0.77±1.13 fmol/mL) in plasma were significantly increased in the CAD group compared with the non-CAD group (all P<0.05).
Conclusions Heavy smoking, hypertension, alcohol consumption, type 2 diabetes mellitus, high-fat diet and BMI>24 kg/m2 were significantly related to CAD in patients aged ≤ 40, with heavy smoking presenting the highest OR. Metabolic syndrome and inflammation were also more common in young CAD patients than in non-CAD patients.