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Biomedical subjects

Huibi Xu

Publications and source records attributed to Huibi Xu.

At least 19 recordsLinked to original sources
PubMed2006

Tumor necrosis factor alpha blocking peptide loaded PEG-PLGA nanoparticles: preparation and in vitro evaluation.

Nanoparticles prepared from polyethyleneglycol-modified poly(d,l-lactide-co-glycolide) (PEG-PLGA-NPs) are being extensively investigated as drug carriers due to their controlled release, biodegradable and biocompatibility. The purpose of this study was to evaluate the in vitro characteristics of PEG-PLGA-NPs loading tumor necrosis factor alpha blocking peptide (TNF-BP). PEG-PLGA copolymer was synthesized by ring-opening polymerization of d,l-lactide, glycolide and methoxypolyethyleneglycol (mPEG) (Mw = 5000). Blank PEG-PLGA-NPs, with particle size within the range of 79.7 to 126.1 nm and zeta potential within the range of -12.91 to -24.55 mV, were prepared by the modified-spontaneous emulsification solvent diffusion (modified-SESD) method. PEG-PLGA-NPs uptake by murine peritoneal macrophages (MPM) was lower than that of PLGA-NPs. TNF-BP was loaded on the blank nanoparticles by electrostatic interactions, and TNF-BP loading capacity of PEG-PLGA-NPs was found to be dependent on the characteristics of blank nanoparticles, peptide concentration and incubation medium. In vitro release experiments showed the peptide release rate affected by the drug loading and ionic strength, and approximately 60.2% of TNF-BP released from nanoparticles still possessed bioactivity. These experimental results indicate that PEG-PLGA-NPs could be used to develop as drug carriers for TNF-BP.

Animals↗
PubMed2006

An attempt to directly trace polymeric nanoparticles in vivo with electron microscopy.

This work attempted to directly observe polymeric nanoparticles in vivo by analytical electron microscopy (AEM) using copper chlorophyll as the contrast agent, based on the experiments concerned with the copper chlorophyll labeled poly-DL-lactide nanoparticles and the in vivo distribution of the polysorbate 80 (T-80)-coated nanoparticles in brain tissues. With the nanoprecipitation method without surfactants, copper chlorophyll is aggregated in the coordinately saturated form and encapsulated by the matrices of nanoparticles, which may ensure the stability of copper chlorophyll during the in vivo experiments. From both morphological information and chemical information, only the labeled nanoparticles with the T-80 coating were directly traced in the brain by AEM. The results not only support the mechanism of endocytosis and/or transcytosis of T-80-coated nanoparticles targeted to the brain but also verify that it is practical to probe polymeric nanoparticles in vivo using AEM together with copper chlorophyll as the contrast agent.

Animals↗
PubMed2006

Isotretinoin-loaded solid lipid nanoparticles with skin targeting for topical delivery.

The purpose of this study was to construct isotretinoin-loaded SLN (IT-SLN) formulation with skin targeting for topical delivery of isotretinoin. PRECIROL ATO 5 was selected as the lipid of SLN. Tween 80 and soybean lecithin were used as the surfactants to stabilize SLN. The hot homogenization method was performed to prepare the drug-loaded SLN. The various formulations were characterized by photon correlation spectroscopy and all the SLN formulations had low average size between 30 and 50 nm. Transmission electron microscopy studies showed that the IT-SLN formulation had a spherical shape. All the formulations had high entrapment efficiency ranging from 80% to 100%. The penetration of isotretinoin from the IT-SLN formulations through skins and into skins were evaluated in vitro using Franz diffusion cells fitted with rat skins. The in vitro permeation data showed that all the IT-SLN formulations can avoid the systemic uptake of isotretinoin in skins, however the control tincture had a permeation rate of 0.76+/-0.30 microg cm(-2)h(-1) through skins. The IT-SLN consisting of 3.0% PRECIROL ATO 5, 4.0% soybean lecithin and 4.5% Tween 80 could significantly increased the accumulative uptake of isotretinoin in skin and showed a significantly enhanced skin targeting effect. The studied IT-SLN showed a good stability. These results indicate that the studied IT-SLN formulation with skin targeting may be a promising carrier for topical delivery of isotretinoin.

Administration, Cutaneous↗
PubMed2006

Microemulsion-based hydrogel formulation of ibuprofen for topical delivery.

The purpose of this study was to construct microemulsion-base hydrogel formulation for topical delivery of ibuprofen. Ethyl oleate (EO) was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems and excellent skin permeation rate of ibuprofen. The pseudo-ternary phase diagrams for microemulsion regions were constructed using ethyl oleate as the oil, Tween 80 as the surfactant, propylene glycol as the cosurfactant. Various microemulsion formulations were prepared and the abilities of various microemulsions to deliver ibuprofen through the skin were evaluated in vitro using Franz diffusion cells fitted with porcine skins. The in vitro permeation data showed that microemulsions increased the permeation rate of ibuprofen 5.72-30.0 times over the saturated solution. The optimum formulation consisted of 3% ibuprofen, 6% EO, 30% Tween 80/PG (2:1) and water, showed a high permeation rate of 38.06 microg cm(-2) h(-1). Xanthan gum as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The studied microemulsion-based hydrogel showed a good stability. These results indicate that the studied microemulsion-based hydrogel may be a promising vehicle for topical delivery of ibuprofen.

Administration, Topical↗
PubMed2006

Effects of flavonoids extracted from Scutellaria baicalensis Georgi on hemin-nitrite-H2O2 induced liver injury.

Hemin-nitrite-H2O2 system may play a role in liver oxidative injury in some pathological events. In this paper, the effects of the three active components of the root of Scutellaria baicalensis Georgi, i.e. baicalin, baicalein and wogonin, on hemin-nitrite-H2O2 induced liver injury were studied in liver homogenate, liver microsome and human hepatoblastoma cell line HepG2 cells. It was found that hemin-nitrite-H2O2 could induce liver homogenate protein nitration, lipid peroxidation and liver microsome protein oxidation; it also caused a decrease of HepG2 cells viability. Baicalein, baicalin and wogonin could inhibit protein nitration and lipid peroxidation in liver homogenate as well as in HepG2 cells in a dose-dependent manner, the inhibition order was baicalein>baicalin>>wogonin. These three flavonoids also inhibited the oxidation of protein in liver microsome, the decrease of cell viability and the content of GSH in HepG2 cells, among which baicalin represented the most inhibitory effect. Besides, hemin-H2O2 induced cell injury could be augmented with the existence of nitrite, indicating protein nitration involved in hemin-nitrite-H2O2 induced liver injury. These results demonstrated hemin-nitrite-H2O2 could induce liver injury through oxidizing or nitrating different biomolecules. Baicalein, baicalin and wogonin could inhibit hemin-nitrite-H2O2 induced liver injury in dose-dependent manners by inhibiting oxidation and nitration.

Animals↗
PubMed2005

Podophyllotoxin-loaded solid lipid nanoparticles for epidermal targeting.

The purpose of this study was to evaluate solid lipid nanoparticles as the topical carrier for epidermal targeting of podophyllotoxin (POD). The high pressure homogenization was employed to prepare drug-loaded solid lipid nanoparticles. The POD-loaded SLN stabilized by 0.5% poloxamer 188 and 1.5% soybean lecithin (P-SLN) and 2% polysorbate 80 (T-SLN) was characterized by photon correlation spectroscopy (PCS). P-SLN showed an average diameter of 73.4 nm and a zeta potential of -48.36 mV. The imaging of AFM indicated that the P-SLN had a spherical shape. DSC and X-ray diffraction analysis showed that POD was dispersed in SLN in an amorphous state. The in vitro permeation study showed that P-SLN increased the accumulative amount of POD in porcine skin 3.48 times over 0.15% tincture. But T-SLN with a diameter of 123.1 nm and a zeta potential of -17.4 mV did not show a high accumulative amount of POD when compared with P-SLN, though both P-SLN and T-SLN could avoid the systemic uptake of POD. Because of the fluorescence property of POD, fluorescence microscopy imaging was employed to visualize the penetration of POD into skin from SLN. The penetration of POD from P-SLN seemed to follow two pathways along the stratum corneum and hair follicle route. The imaging revealed that P-SLN had a strong localization of POD within epidermis. The penetration of P-SLN with low particle size into stratum corneum along the skin surface 'furrow' and the consequent controlled release of POD might lead to the epidermal targeting. P-SLN provides a good epidermal targeting effect and may be a promising carrier for topical delivery of POD.

Animals↗
PubMed2005

Effects of Erigeron breviscapus ethanol extract on neuronal oxidative injury induced by superoxide radical.

Antioxidant activity of the ethanol extract of Erigeron breviscapus (EEEB) were studied by using neuron oxidative injury model induced by superoxide radical. EEEB at the dose of 10-140 mug/ml reduced significantly the lipid peroxidation levels and lactic dehydrogenase (LDH) release from neuron exposed to superoxide radical (generated by xanthine and xanthine oxidase). These results suggest that neuroprotective actions of EEEB may be due to its antioxidant or radical scavenging activity.

Animals↗
PubMed2005

Effects of amino acids from selenium-rich silkworm pupas on human hepatoma cells.

Selenium (Se) plays an important role in cancer-prevention. Silkworm pupas have been used as a Chinese traditional medicine since ancient time. In order to find effective carcinostatic agents, Se-rich amino acids were extracted from Ziyang silkworm pupas. The Se content of Ziyang pupas was measured to be 215 times higher than that of Luoyang normal ones, and the majority of Se was stored in proteins. Composition analysis showed that Se-rich amino acids from Ziyang pupas had higher amounts of selenomethionine, methionine, cystine, and tyrosine than normal amino acids from Luoyang pupas which were rich in amino acids containing alkyl side chains. When cultured with human hepatoma cells SMMC-7721, Se-rich amino acids at concentrations of 0.5, 1.5, and 2.5 micromol L(-1) Se significantly and dose-dependently inhibited cell viability, induced changes in cell morphology and cycle, and caused cell apoptosis. On the contrary, normal amino acids did not show any inhibitory effect on SMMC-7721 cells. Sodium selenite or selenomethionine at the same Se concentrations only slightly inhibited the hepatoma cells. Mechanism study showed that selenium-rich amino acids could increase the generation of intracellular reactive oxygen species (ROS) concentration-dependently. Antioxidant N-acetylcyteine partially inhibited the increase of ROS. Those results suggested that Se-rich amino acids were effective carcinostatic agents compared with sodium selenite and selenomethionine. The mechanism for their hepatoma-inhibitory effects was the induction of cellular apoptosis through ROS generation.

Amino Acids↗
PubMed2005

Effects of dietary baicalin supplementation on iron overload-induced mouse liver oxidative injury.

Iron overload is one of the most common metal related toxicity. Under this circumstance, excessive iron deposition in liver will lead to further injury such as hepatocellular necrosis, inflammation, fibrosis, and in some cases even to carcinoma. In this paper, the effect of a nature flavonoid, baicalin, on iron overload-induced mouse liver oxidative injury has been studied. It was found that when iron-dextran-induced iron overload, mice were fed baicalin-containing diet (0.25% and 1%) for 50 days, hepatic iron, liver-to-body weight ratio, and hepatic lipid peroxidation were dose-dependently decreased; while catalase activity, total antioxidant status, and serum iron content were dose dependently increased. The protective effect of baicalin on liver of iron overload mouse may due to both the antioxidant and iron chelation activities of baicalin. These data provide preliminary experimental support for baicalin as medicine for iron overload diseases.

Animals↗
PubMed2005

Anti-inflammatory effects of triptolide loaded poly(D,L-lactic acid) nanoparticles on adjuvant-induced arthritis in rats.

Triptolide (TP), which has potent immunosuppressive effects, anti-inflammatory and severe toxicity on digestive, urogenital, blood circulatory system, was used as a model drug in this study. The aim of this study was to investigate the anti-inflammatory effect of complete Freund's adjuvant-induced arthritis in rats treated with TP-loaded poly(D,L-lactic acid) (PLA) nanoparticles (TP-PLA-NPs) by gavage. TP-PLA-NPs were prepared by the modified spontaneous emulsification solvent diffusion method (modified-SESD). Nanoparticles were shown to be small particle size (149.7 nm), low polydispersity index (0.088), a fine spherical shape with smooth surfaces determined by dynamic light scattering (DLS) and transmission electron microscope (TEM). Encapsulation efficiency and the in vitro release of TP from nanoparticles were measured by the reverse phase high-performance liquid chromatography (RP-HPLC). The in vitro release profile of TP from nanoparticles exhibited a typical biphasic release phenomenon, namely initial burst release and consequently slow release. The potential therapeutic arthritic method of TP-PLA-NPs was established. The results obtained in experiments indicated that TP-PLA-NPs significantly inhibited the adjuvant-induced arthritis, and had preferable anti-inflammatory effect with the long-time administration.

Animals↗
PubMed2005

Effect of scutellarin on nitric oxide production in early stages of neuron damage induced by hydrogen peroxide.

The aims of the present study were to investigate the regulatory function of scutellarin on production of nitric oxide (NO) as well as activities of constitutive NO synthase (cNOS) and inducible NO synthase (iNOS) in early stages of neuron damage induced by hydrogen peroxide. Direct detection of NO production was performed on primary cultures of living rat neuronal cells with an electrochemical sensor. Hydrogen peroxide significantly increased culture supernatant levels of NO, the total integral value of the defined areas (500-6500 sxpA) reached 3.68 x 10(6). Pre-treatment with scutellarin, caused the total integral value to decrease in a dose-dependent fashion (3.24 x 10(6), 2.15 x 10(6), 1.84 x 10(6) for groups 10, 50, and 100 uM scutellarin, respectively). After exposure to 2.0mM hydrogen peroxide for 2h, malondialdehyde (MDA) level, a marker of lipid peroxidation, was remarkably increased. The elevation can be suppressed by scutellarin. Hydrogen peroxide also caused significant loss of neuron viability. In comparison with the control group, scutellarin significant attenuated the loss. Results also showed that hydrogen peroxide increased activity of cNOS, which was markedly inhibited by scutellarin. However, exposure of neuronal cells to hydrogen peroxide did not lead to an increase in iNOS activity. In conclusion, our results suggest that NO production, which increased in early stages of neuron damage induced by hydrogen peroxide can be effectively inhibited by scutellarin. Moreover, our results indicate that increase in NO production is mediated by cNOS.

Animals↗
PubMed2005

Oleanolic acid nanosuspensions: preparation, in-vitro characterization and enhanced hepatoprotective effect.

Oleanolic acid is a naturally derived triterpene used clinically in the treatment of hepatitis in China, but its poor solubility often leads to poor bioavailability. In the present study, oleanolic acid nanosuspensions were prepared by the nanoprecipitation method and then systematically characterized. The average particle size of the obtained nanosuspensions was 284.9 nm, with a polydispersity index of 0.216. Transmission electron microscopy and atomic force microscopy showed that the drug existed as spherical or near-spherical nanoparticles in the nanosuspensions. Differential scanning calorimetry and X-ray diffraction studies indicated that oleanolic acid was present in an amorphous state in the lyophilized nanosuspensions. At 25 degrees C, the saturation solubility of oleanolic acid was increased by about 6 times after nanoation (25.72 microg mL(-1) vs 4.37 microg mL(-1)). In the in-vitro drug release experiments, the lyophilized nanosuspensions showed a faster drug dissolution rate than that of the coarse drug powder (approx. 90% vs 15% during the first 20 min), and nearly 95% of the oleanolic acid was released by 120 min. As evidenced by the lower serum alanine aminotransferase activity and liver malondialdehyde content, pre-treatment with oleanolic acid nanosuspensions significantly enhanced the hepatoprotective effect of oleanolic acid against carbon tetrachloride-induced liver injury.

Administration, Oral↗
PubMed2004

Hemin/nitrite/H2O2 induces brain homogenate oxidation and nitration: effects of some flavonoids.

Oxidative injury has been implicated in the pathogenesis of numerous neurodegenerative diseases. Recently, it has been found that with the existence of hydrogen peroxide and nitrite, hemin catalyzes protein nitration. We hypothesize under certain pathological conditions, hemin catalyzed protein nitration may happen in the brain. In this paper, the effects of three flavonoids, i.e. quercetin, catachin and baicalein on hemin/nitrite/H2O2 induced brain homogenate oxidation and nitration were studied. The results showed that hemin/nitrite/H2O2 system could effectively induce brain homogenate protein oxidation and nitration. Quercetin, catachin and baicalein dose-dependently inhibited hemin/nitrite/H2O2 system-induced protein nitration in a dose-dependent manner, the inhibition of protein nitration was in the order of quercetin>catachin>baicalein. These compounds also inhibited hemin/H2O2 system-induced lipid peroxidation, the inhibition order was baicalein >quercetin>catachin. However, these flavonoids showed marginal effect on hemin/nitrite/H2O2 system caused protein oxidation and thiol oxidation. The inhibition activities of flavonoids on hemin/nitrite/H2O2 system-induced protein nitration may closely relate to their radical scavenging activities, since the inhibition order of protein nitration is the same as the radical scavenging order. These results indicate hemin/nitrite/H2O2 system induces different types of oxidative assault on bio-molecules. Flavonoids could act as antioxidants inhibiting ROS and RNS caused brain damage.

Animals↗
PubMed2004

A study of microemulsion systems for transdermal delivery of triptolide.

Triptolide possesses immunosuppressive, anti-fertility and anti-cancer activities. Due to its severe toxicity, microemulsions with controlled, sustained and prolonged delivery of triptolide via a transdermal route are expected to reduce its adverse side effects. The purpose of the present study was to investigate the microemulsions for transdermal delivery of triptolide. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using oleic acid as an oil, Tween 80 as a surfactant and propylene glycol as a cosurfactant. The droplet size of microemulsions was characterized by photocorrelation spectroscopy. The transdermal ability of triptolide from microemulsions was evaluated in vitro using Franz diffusion cells fitted with mouse skins and triptolide was analyzed by high-performance liquid chromatography. The effect of menthol as a permeation enhancer, and the loading dose of triptolide in microemulsions on the permeation rate were also evaluated. The triptolide-loaded microemulsions showed an enhanced in vitro permeation through mouse skins compared to an aqueous solution of 20% propylene glycol containing 0.025% triptolide. The permeation of microemulsions accorded with the Fick's first diffusion law. No obvious skin irritation was observed for the studied microemulsion ME6, but the aqueous solution of 20% propylene glycol containing 0.025% triptolide revealed the significant skin irritation. The results indicate that the studied microemulsion systems, especially ME6, may be promising vehicles for the transdermal delivery of triptolide.

Administration, Cutaneous↗
PubMed2004

Effects of trace elements on the telomere lengths of hepatocytes L-02 and hepatoma cells SMMC-7721.

The effects of selenium, zinc, iron, chromium, and lead on telomere lengths of human cells have not been investigated. This article adopted flow cytometry and fluorescence in situ hybridization to investigate the impact of different elements on cellular apoptosis and telomere lengths of human hepatocytes L-02 and hepatoma cells SMMC-7721. Results showed that these trace elements under the following dosages did not have remarkable effect on cellular apoptosis. However, sodium selenite at doses of 0.5 and 2.5 micromol/L significantly extended the telomere length of hepatocytes L-02; 0.5 micromol/L lead acetate remarkably shortened the telomere length of L-02 cells; 80 micromol/L zinc sulfate, 20 micromol/L ferric chloride, and 200 micromol/L chromic chloride only had slight impact on the telomere length, respectively. Regarding hepatoma cells SMMC-7721, sodium seleite at 0.5 and 2.5 micromol/L had little impact on the telomere length; 80 micromol/L zinc sulfate significantly accelerated the loss of telomere length, whereas 20 micromol/L ferric chloride, 200 micromol/L chromic chloride, and 0.5 micromol/L lead acetate remarkably extended the telomere lengths, respectively. The results revealed differential effects of each trace element on the life-span of human hepatocytes and hepatoma cell lines, which suggested further research on somatic hepatocytes and hepatoma in vivo.

Apoptosis↗
PubMed2004

Antagonistic effect of scutellarin on the toxicity of selenium in rat livers.

Selenium has both nutritional function and toxicity according to its concentration and species. To counteract the toxicity of selenium, scutellarin was investigated. Wistar rats were supplemented with 40 microg Se/kg/d as sodium selenite, 40 microg Se/kg/d with 20 mg/kg/d scutellarin, and 20 mg/kg/d scutellarin, respectively, for 15 d. The mRNA levels and activities of glutathione peroxidase (GSH-Px) and thioredoxin reductase (TR), and the malondialdehyde (MDA) contents were measured. Reactive oxygen species (ROS) were detected by chemiluminescence assay, and tissue conformation was investigated by histological study. The results showed significant decreases of mRNA levels and activities of GSH-Px and TR and a significant increase of MDA content in livers of the Se-treated rats (p<0.05, compared with the control). Supplementation of scutellarin to the Se-treated group significantly inhibited the decreases of mRNA levels and activities, and the increase of MDA content (p<0.05, compared with the Se-treated group). Meanwhile, scutellarin-scavenged ROS generated in the mixture of sodium selenite, reduced glutathione, and oxygen. Liver injury was displayed in slices exposed to selenium at the present dose. The groups treated with both selenium and scutellarin or only scutellarin did not show significant tissue damage. Thus, scutellarin had an antagonistic effect against the toxicity of selenium.

Animals↗
PubMed2003

Both calcium and ROS as common signals mediate Na(2)SeO(3)-induced apoptosis in SW480 human colonic carcinoma cells.

Recent studies have shown that reactive oxygen species (ROS) play a crucial role in Se-induced cell apoptosis. A number of studies have demonstrated that perturbed cellular calcium homeostasis has been implicated in apoptosis. The main objective of this study was to evaluate the role of Ca(2+) in Na(2)SeO(3)-induced apoptosis and the relationship between Ca(2+) and ROS in human colonic carcinoma cells SW480. When SW480 cells were exposed to 25-100 microM Na(2)SeO(3), both cell apoptosis and growth inhibition were observed by flow cytometric analysis and 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay. Na(2)SeO(3) was able to induce increase of [Ca(2+)](i) and ROS production and disrupt mitochondrial membrane potential (Delta Psi m) in SW480 cells monitored by using a confocal laser scanning microscope. Ca(2+) channel inhibitor CoCl(2) and an intracellular Ca(2+) chelator o-phtalaldehyde, 1,2-bis(2-aminophenoxy)-ethane-N,N,N',N'-tetra-acetic acid acetoxymethyl ester (BAPTA) completely inhibited [Ca(2+)](i) increase, but catalase had no effect on Na(2)SeO(3)-induced increase of [Ca(2+)](i). BAPTA-AM, CoCl(2), and mitochondrial Ca(2+) uptake inhibitor ruthenium red blocked Delta Psi m dissipation. The increase of ROS was also suppressed by CoCl(2), BAPTA, ruthenium red, N-acetylcysteine and catalase, respectively. The mitochondrial uncoupler carbonyl cyanide p-(trifluoromethoxy) phenylhydrazone (FCCP) completely inhibited Na(2)SeO(3)-induced ROS increase. This showed that ROS increase is due to mitochondrial Ca(2+) overload. The Na(2)SeO(3)-induced apoptosis of SW480 cells was also inhibited by CoCl(2), BAPTA, ruthenium red, N-acetylcysteine, and catalase, respectively. The results mentioned above imply that both calcium and Ca(2+)-dependent ROS as a signal molecule mediate apoptosis induced by Na(2)SeO(3) in SW480 cells.

Acetylcysteine↗