A novel oral delivery system that TPGS modified docetaxel proniosomes, DTX-TPGS-PN, was developed and the characterization after hydration was observed. Firstly, Doce-TPGS-PN was optimized by investing the factors, including the type of surfactant, methods of adding TPGS, content of TPGS and the molar ratio of span40/cholesterol, which may affecting the particle size, encapsulation efficiency and instantaneous release of drug in the formulation. Then, the morphology, particle size, Zeta potential, encapsulation efficiency and in vitro release of the formulation were evaluated. The result showed that hydrated nanoparticles of DTX-TPGS-PNs were (93 ± 6.5) nm in size,(-83.95 ± 3.69) mV in zeta potential, (97.31 ± 0.60)% in encapsulation efficiency, exhibiting spherical morphology and biphasic release process that a low burst effect within the first 0.5 hour and a relative-sustained release for the next several hours in PBS. These results indicate the oral delivery system of DTX-TPGS-PN was successfully built with good properties.
Chemistry, Pharmaceutical ; methods ; Particle Size ; Polyethylene Glycols ; chemistry ; Taxoids ; chemistry ; pharmacology ; Vitamin E ; analogs & derivatives ; chemistry

OBJECTIVETo provide foundation for developing Gynostemma pentaphyllum with physic and edible use.

METHODTo plant the seven leaves with sweet taste of Enshi, Five leaves with honey taste of Enshi, Makino (picric taste) taste, in the same ecological environment in accordance with the require of mathematical statistics and give the same management, At the same time, sowing and reaping dry grass to do composition analysis;

RESULTThe ginseng total saponin, the total amino acid. VitE, VitB1, VitB2 of the two new variety are 33% and 34.3%, 11.8% and 4.7%, 76% and 45.8%, 46% and 76.1%, 41.2% and 25% higher than the raw variety of Gynostemma pentaphyllam Makino respectively. All of them achieve the remarkable standard. The total sugar of the two is 16.3% and 4.4% lower than the raw variety of G. pentaphyllum respectively.

CONCLUSIONThe two new variety is not only with the distinct flavor and good taste, but also has wider used domain More amount of utilization, Better medical treatment and health care than the raw variety of G. pentaphyllum. It is more worthful to develop in industry domain.

Amino Acids ; analysis ; Carbohydrates ; analysis ; Genetic Variation ; Ginsenosides ; analysis ; Gynostemma ; chemistry ; genetics ; Plants, Edible ; chemistry ; genetics ; Plants, Medicinal ; chemistry ; genetics ; Riboflavin ; analysis ; Thiamine ; analysis ; Vitamin E ; analysis

OBJECTIVETo investigate the changes of the levels of galectin-3 (Gal-3) in serum and bronchoalveolar lavage fluid (BALF) of children with asthma whose have different serum levels of 25-hydroxyl-vitamin D₃[25(OH)D₃].

METHODSFifty children with asthma between January 2013 and December 2014 were enrolled as the asthma group, and they were classified into 25(OH)D₃sufficient (n=7), insufficient (n=12) and deficient subgroups (n=31) according to the serum levels of 25(OH)D₃. Twenty children with abnormal airway or tracheal foreign bodies served as the control group. The levels of 25(OH)D₃, Gal-3 and total IgE in serum and Gal-3 levels in BALF were measured using ELISA.

RESULTThe serum levels of 25(OH)D₃in the asthma group were lower than in the control group (P<0.05). The 25(OH)D₃deficient subgroup displayed the highest percentages of neutrophils, eosinophils and epithelial cells in BALF, followed by the 25(OH)D₃insufficient subgroup and the 25(OH)D₃sufficient subgroup (P<0.05). The percentages of neutrophils, eosinophils and epithelial cells in BALF in the three subgroups were all higher than in the control group (P<0.05). In children with asthma, serum levels of 25(OH)D₃were negatively correlated with the percentages of neutrophils, eosinophils and epithelial cells in BALF (r=-0.683, -0.795 and -0.670 respectively; P<0.05); and a negative correlation was also seen between serum 25(OH)D₃levels and serum Gal-3 and total IgE levels (r=-0.759 and -0.875 respectively; P<0.05).

CONCLUSIONSThe children with asthma have low serum levels of 25(OH)D₃. 25(OH)D₃and Gal-3 may be involved in the airway inflammation and the development of asthma.

Asthma ; etiology ; metabolism ; Bronchoalveolar Lavage Fluid ; chemistry ; Child ; Child, Preschool ; Female ; Galectin 3 ; analysis ; blood ; physiology ; Humans ; Immunoglobulin E ; blood ; Infant ; Male ; Vitamin D ; analogs & derivatives ; blood ; physiology

V(E) acetate-loaded methoxy poly(ethylene glycol)-b-poly(lactic acid) amphiphilic diblock copolymer nano-dispersion (PMV) was prepared by self-emulsification/solvent evaporation method. The drug-loaded amount, size distribution of PMV nanoparticles, and entrapment efficiency of V(E) acetate (V(E)A) were determined by UV and laser particle analyzer. Drug release in vitro was primarily investigated by UV. The results indicate that the size of PMV nanoparticles is less than 300 nm and PMV is largely influenced by preparation methods, property of solvents, V(E)A-fed amount, and the concentration of dispersion. The initial burst release is not observed and the accumulated release is more than 79% after 14 h. This study develops a new formulation for V(E)A and provides an experimental basis for the novel drug delivery systems of V(E)A.
Delayed-Action Preparations ; chemical synthesis ; Drug Carriers ; administration & dosage ; chemistry ; Hydrophobic and Hydrophilic Interactions ; Nanoparticles ; Polyesters ; administration & dosage ; Polyethylene Glycols ; administration & dosage ; Vitamin E ; administration & dosage

Hesperetin, an abundant bioactive component of citrus fruits, is poorly water-soluble, resulting in low oral bioavailability. We developed new formulations to improve the water solubility, antioxidant activity, and oral absorption of hesperetin. Two nano-based formulations were developed, namely hesperetin-TPGS (D-α-tocopheryl polyethylene glycol 1000 succinate) micelles and hesperetin-phosphatidylcholine (PC) complexes. These two formulations were prepared by a simple technique called solvent dispersion, using US Food and Drug Administration (FDA)-approved excipients for drugs. Differential scanning calorimetry (DSC) and dynamic light scattering (DLS) were used to characterize the formulations' physical properties. Cytotoxicity analysis, cellular antioxidant activity assay, and a pharmacokinetic study were performed to evaluate the biological properties of these two formulations. The final weight ratios of both hesperetin to TPGS and hesperetin to PC were 1:12 based on their water solubility, which increased to 21.5- and 20.7-fold, respectively. The hesperetin-TPGS micelles had a small particle size of 26.19 nm, whereas the hesperetin-PC complexes exhibited a larger particle size of 219.15 nm. In addition, the cellular antioxidant activity assay indicated that both hesperetin-TPGS micelles and hesperetin-PC complexes increased the antioxidant activity of hesperetin to 4.2- and 3.9-fold, respectively. Importantly, the in vivo oral absorption study on rats indicated that the micelles and complexes significantly increased the peak plasma concentration (C_max) from 2.64 μg/mL to 20.67 and 33.09 μg/mL and also increased the area under the concentration-time curve of hesperetin after oral administration to 16.2- and 18.0-fold, respectively. The micelles and complexes increased the solubility and remarkably improved the in vitro antioxidant activity and in vivo oral absorption of hesperetin, indicating these formulations' potential applications in drugs and healthcare products.
Administration, Oral ; Animals ; Antioxidants/chemistry* ; Biological Availability ; Calorimetry, Differential Scanning ; Dogs ; Dose-Response Relationship, Drug ; Drug Carriers ; Female ; Hep G2 Cells ; Hesperidin/chemistry* ; Humans ; Light ; Madin Darby Canine Kidney Cells ; Micelles ; Phosphatidylcholines/chemistry* ; Polyethylene Glycols/chemistry* ; Rats ; Rats, Sprague-Dawley ; Scattering, Radiation ; Solubility ; Solvents ; Vitamin E/chemistry* ; Water/chemistry* ; alpha-Tocopherol/chemistry*

OBJECTIVETo observe the effects of ginkgo flavone aglycone (GA) on oxidized low-density lipoprotein (ox-LDL) induced oxidative injury of human aortic endothelial cells (HAECs) and its mechanisms.

METHODSHAECs were in vitro cultured. Then they were divided into 6 groups, i.e., the vehicle control group, the ox-LDL group, the GA 30 mg/L group, the GA 60 mg/L group, the GA 90 mg/L group, and the Vit E group. The oxidative injury model was duplicated in the rest 5 groups by adding 150 mg/L ox-LDL except the vehicle control group. GA was added as intervention at corresponding dose to the GA 30 mg/L group, the GA 60 mg/L group, and the GA 90 mg/L group. Vit E at 200 micromol/L was administered to those in the Vit E group. The survival rate of HAECs was detected by MTT. The contents of reactive oxygen species (ROS) in HAECs were determined by CM-H2DCFDA fluorescent probe. The contents of NADPH oxidase were detected by ELISA. The levels of malondialdehyde (MDA) were measured by thiobarbituric acid (TBA) test. The contents of nitric oxide (NO) were determined by Griess reagent method. The contents of superoxide dismutase (SOD) were detected by xanthine oxidase method.

RESULTSCompared with the vehicle control group (100.00%), the cell survival rate in the ox-LDL group (70.68%) obviously decreased (P <0.05). The cell survival rate was 88. 95% in the VitE group, 83.25% in the GA 30 mg/L group, and 94.93% in the GA 60 mg/L group, obviously higher than that of the ox-LDL group (70.68%, P <0.05). The optimal effects were shown in the GA 60 mg/L group. Compared with the vehicle control group, the contents of ROS, MDA, and NADPH oxidase increased, the contents of NO and the SOD activity decreased in the ox-LDL group, showing statistical difference (P <0.05). Compared with the ox-LDL group, the contents of ROS, MDA, and NADPH oxidase decreased, the NO content and the SOD activity increased in the GA 30 mg/L group, the GA 60 mg/L group, and the Vit E group, showing statistical difference (P <0.05). The optimal effects were shown in the GA 60 mg/L group.

CONCLUSIONSGA could obviously inhibit ox-LDL induced synthesis of ROS, lower the contents of MDA, and elevate the levels of NO. Its mechanisms might be associated with increasing the activity of SOD and lowering the activity of NADPH oxidase.

Aorta ; cytology ; Cells, Cultured ; Endothelial Cells ; drug effects ; metabolism ; Ginkgo biloba ; chemistry ; Humans ; Isoflavones ; pharmacology ; Lipoproteins, LDL ; pharmacology ; Malondialdehyde ; metabolism ; Nitric Oxide ; metabolism ; Oxidation-Reduction ; Oxidative Stress ; drug effects ; Reactive Oxygen Species ; metabolism ; Superoxide Dismutase ; metabolism ; Vitamin E ; pharmacology

OBJECTIVETo study the changes of nitric oxide (NO) in the BALB/c hairless mice skin after trichloroethylene (TCE) irritation and the protection of ginkgo biloba extract (GbE) and vitamin E (VE).

METHODS132 BALB/c hairless mice were randomly divided into blank control group, solvent group (olive oil), TCE groups (20%TCE, 40%TCE, 80%TCE and 100%TCE), GbE groups (0.1%GbE, 1%GbE and 10%GbE) and VE groups (5%VE, 10% VE and 20% VE), with 11 animals in each group, 5 for acute irritation test and 6 for the cumulative irritation test. The skin irritation was observed, and the levels of NO in the dorsal skin of BALB/C hairless mice were detected. The kit of NO was used to detect the levels of NO in the dorsal skin of BALB/c hairless mice.

RESULTS(1) The skin presented erythema and edema after TCE irritation both in acute irritation and cumulative irritation test and the skin inflammation showed time-dose effect relationship; the mice skin was protected in GbE or VE groups. (2) In the acute stimulation test, the levels of NO in 80%TCE group (69.895 +/- 9.605 micromol/mg pro) and 100%TCE group (77.273 +/- 9.290 micromol/mg pro) were significantly different compared with blank control group and solvent control group (P < 0.05 or P < 0.01). In the protection group, the NO level were reduced, with the statistically significant differences. (3) In acute irritation test, the levels of NO in 80%TCE group (60.362 +/- 9.817 micromol/mg pro) and 100%TCE group (68.027 +/- 9.354 micromol/mg pro) were significantly different compared with blank control group and solvent control group, (P < 0.05 or P < 0.01); In the protection group, 1% GbE, 10% GbE, 10% VE and 20%VE could reduce the levels of NO, with statistically significant differences.

CONCLUSIONTCE can produce the irritation on the dorsal skin of BALB/c hairless mice and induce the significant increase of the NO levels. GbE and VE can protect the skin from TCE irritation damage.

Animals ; Female ; Ginkgo biloba ; chemistry ; Mice ; Mice, Hairless ; Mice, Inbred BALB C ; Nitric Oxide ; metabolism ; Plant Extracts ; pharmacology ; Skin ; drug effects ; metabolism ; Skin Irritancy Tests ; Trichloroethylene ; toxicity ; Vitamin E ; pharmacology

OBJECTIVETo observe the effects of fruit juices with different antioxidant capacity on antioxidant system function of aged rats.

METHODSThirty Wistar rats were randomly divided into three groups: pomegranate juice and apple juice as two experimental groups, while distilled water as normal control group. They were administrated fruit juices or distilled water respectively by gavage daily for 4 weeks. At the end of experiment, the antioxidant system function was assessed.

RESULTSThe aged rats in pomegranate juice group showed significantly higher serum antioxidant capacity (0.90 +/- 0.13) mmol/L than that in control group (0.79 +/- 0.10) mmol/L (P < 0.05). The concentrations of serum carbonyl and oxLDL were decreased significantly in pomegranate juice group as compared to the control group (P < 0.05). The percentage of injured blood lymphocyte DNA and the ratio of tail length/total length were declined significantly in pomegranate juice group (P < 0.05 and P < 0.01 respectively). The apple juice showed no effects except decreased ratio of tail length/total length of injured lymphocyte DNA. There were no changes in concentrations of serum vitamin C, vitamin E, urinary 8-OH-dG excretion and the activities of serum SOD, GSH-Px, CAT among three groups.

CONCLUSIONSThe pomegranate juice should possess higher antioxidant capacity and might improve the antioxidant system function of aged rats, while the apple juice is relatively lower in antioxidant capacity and not very effective. The polyphenols in pomegranate juice might be the important functional components.

Aging ; Animals ; Antioxidants ; administration & dosage ; chemistry ; metabolism ; Ascorbic Acid ; blood ; Beverages ; Catalase ; blood ; Comet Assay ; Female ; Fruit ; chemistry ; Glutathione Peroxidase ; blood ; Lymphocytes ; metabolism ; Male ; Malondialdehyde ; blood ; urine ; Malus ; chemistry ; Punicaceae ; chemistry ; Random Allocation ; Rats ; Rats, Wistar ; Superoxide Dismutase ; blood ; Vitamin E ; blood

OBJECTIVETo investigate the effect of compound Danshen Dripping Pill (CDDP) on peripheral arterial intima-media thickness (IMT) in patients newly diagnosed as type 2 diabetes mellitus.

METHODSOne hundred and eight patients were equally randomized into 3 groups, in addition to the basic hypoglycemic, hypotensive and lipid-regulation treatment, they were administered orally with aspirin (0.1 g, once daily), vitamin E (0.1 g, twice daily) and CDDP (10 pills, thrice daily) for 18 months, respectively. The conventional cardiovascular risk factors, such as hyperglycemia, lipids profile, and homeostasis model assessment of insulin resistance (HOMA-IR) as well as ultrasound measurement of peripheral arterial IMT before and after treatment were compared.

RESULTSIn the group treated with CDDP after treatment, the levels of HbA1c, serum total cholesterol and low density lipoprotein cholesterol (LDL-C) were significantly lower (all P<0.01), HOMA-IR was higher than those in the other two groups; while IMTs of carotid, iliac and femoral arteries were insignificantly different among them (P>0.05); however, the increment of carotid IMT in the CDDP treated group was less than that in the aspirin treated group (P<0.05), and that of femoral IMT was less than both the aspirin and vitamin E treated groups (P<0.05).

CONCLUSIONFor the patients with newly diagnosed type 2 diabetes, additional administration of CDDP to the conventional treatment could exert beneficial effects on blood glucose controling, and lipid profile improvement and delay of arterial intima-media proliferation.

Adult ; Aged ; Aspirin ; therapeutic use ; Blood Glucose ; analysis ; Carotid Intima-Media Thickness ; Cholesterol ; blood ; Diabetes Mellitus, Type 2 ; drug therapy ; pathology ; Diabetic Angiopathies ; prevention & control ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Insulin Resistance ; Male ; Middle Aged ; Phenanthrolines ; therapeutic use ; Phytotherapy ; Salvia miltiorrhiza ; chemistry ; Vitamin E ; therapeutic use

Brown algae are well known as a source of biologically active compounds, especially those having antioxidant activities, such as phlorotannins. In this study we examined the antioxidant activities of crude phlorotannins extracts (CPEs) obtained from Sargassum hemiphyllum (SH) and fractionated according to the molecular weights. When CPEs were administrated at a dose of 30 mg/kg to Kunming mice pre-treated with carbon tetrachloride (CCl4), the levels of oxidative stress indicators in the liver, kidney and brain were significantly reduced in vivo. All the components of various molecular weight fractions of CPEs exhibited greater scavenging capacities in clearing hydroxyl free radical and superoxide anion than the positive controls gallic acid, vitamin C and vitamin E. Particularly, the components greater than 30 kD obtained from ethyl acetate phase showed the highest antioxidant capacities. These results indicated that SH is a potential source for extracting phlorotannins, the algal antioxidant compounds.
Animals ; Antioxidants ; isolation & purification ; pharmacology ; Ascorbic Acid ; pharmacology ; Brain ; drug effects ; metabolism ; pathology ; Carbon Tetrachloride ; antagonists & inhibitors ; toxicity ; Carbon Tetrachloride Poisoning ; drug therapy ; metabolism ; pathology ; Chemical Fractionation ; methods ; Gallic Acid ; pharmacology ; Hydroxyl Radical ; antagonists & inhibitors ; metabolism ; Kidney ; drug effects ; metabolism ; pathology ; Liquid-Liquid Extraction ; methods ; Liver ; drug effects ; metabolism ; pathology ; Male ; Mice ; Mice, Inbred Strains ; Oxidation-Reduction ; Oxidative Stress ; drug effects ; Phaeophyta ; chemistry ; Sargassum ; chemistry ; Superoxides ; antagonists & inhibitors ; metabolism ; Tannins ; isolation & purification ; pharmacology ; Vitamin E ; pharmacology