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1.
BMC Med Educ ; 24(1): 473, 2024 Apr 29.
Article in English | MEDLINE | ID: mdl-38685015

ABSTRACT

BACKGROUND: Studies has suggested that receiving social support improves the professional identity of health professional students. According to the two-way social support theory, social support includes receiving social support and giving social support. However, the effect of the two-way social support on health professional students' professional identity has not been clarified yet. METHODS: To explore the mechanism of how two-way social support affects health professional students' professional identity, an observational, cross-sectional study was conducted among a convenience and cluster sample of 1449 health professional students from two medical schools in western China. Measures included a short version of the two-way social support scale, a health professional students' professional identity questionnaire, an achievement motivation scale, and a meaning in life scale. Data were analyzed by use of SPSS26.0 software and PROCESSv4.0 plug-in. RESULTS: Receiving social support, giving social support, achievement motivation, meaning in life, and professional identity were positively correlated with each other. Receiving and giving social support not only directly predicted health professional students' professional identity, but also indirectly predicted health professional students' professional identity through the mediating roles of achievement motivation and meaning in life, and the chain mediating roles of achievement motivation and meaning in life, respectively. The effectiveness of predicting health professional students' professional identity varied among different types of two-way social support, which could be depicted as two-way social support > mainly giving social support > mainly receiving social support > low two-way social support. CONCLUSION: In the medical education, the awareness and ability of health professional students to receive and give social support should be strengthened. More attention should be drawn on the chain mediating effect of achievement motivation and meaning in life between two-way social support and professional identity. The current results shed new light on exploring effective ways of improving health professional students' professional identity, which suggested that more attention should be paid to the positive effects of mainly giving social support and two-way social support rather than only on the effects of receiving social support.


Subject(s)
Motivation , Social Identification , Social Support , Humans , Cross-Sectional Studies , Male , Female , Young Adult , China , Students, Medical/psychology , Adult , Surveys and Questionnaires , Students, Health Occupations/psychology
2.
Yao Xue Xue Bao ; 52(1): 139-45, 2017 01.
Article in Chinese | MEDLINE | ID: mdl-29911813

ABSTRACT

Polyamidoamine (PAMAM) dendrimers as synthetic gene vectors are efficient gene delivery systems. In this study, a kind of α-cyclodextrin-PAMAM conjugates polymer (Cy D-G1) was synthesized as a gene delivery vector. Based on ~1H NMR detectation, about 6.4 PAMAM-G1 molecules was grafted onto an α-CD core. Agarose gel electrophoresis revealed that Cy D-G1 could efficiently bind with DNA to condense them into nano-scale particles, which showed a similar binding capacity of PEI-25 K. Besides, it could protect DNA from DNase I degradation in a low N/P ratio. When N/P ratio in the CyD-G1/DNA polyplex was 40, the average particle size of CyD-G1/DNA polyplex was about 120 nm, and zeta potential was +21 mV. This polyplex could maintain its particle size in serum-containing solution within 360 min. In comparison with PEI-25 K carrier, CyD-G1 showed low cytotoxicity in various cell lines. Cell transfection results showed that CyD-G1 efficiently delivered DNA into cells at N/P = 80 compared with Lipofectamine 2000 and PEI-25 K. Unlike Lipofectamine 2000 and PEI-25 K, in serum-containing test condition, CyD-G1/DNA polyplex could maintain the transgene activities. The results of confocal laser scanning microscopy indicated that most DNA entered into cell nuclei within 4 h, and this phenomenon was consistent with the results calculated by flow cytometry. Taken together, CyD-G1 showed good transgene activities and the gene delivery vector could be used not only in vitro but also in vivo.


Subject(s)
Gene Transfer Techniques , Genetic Vectors , Polyamines/chemistry , alpha-Cyclodextrins/chemistry , Cations , Cell Line , DNA , Dendrimers/chemistry , Electrophoresis, Agar Gel , Humans , Lipids , Particle Size , Polymers , Serum , Transfection , Transgenes
3.
J Biomater Sci Polym Ed ; 23(5): 677-95, 2012.
Article in English | MEDLINE | ID: mdl-21375808

ABSTRACT

A non-viral gene-delivery system has been used to deliver plasmid DNA into specific cell types because of its safety and ease of manufacture. Receptor-mediated gene transfer is currently a promising gene-delivery technique. To specifically target genes to asialoglycoprotein receptor of hepatocytes, a galactose moiety was combined into the poly(ethylene glycol) (PEG)-terminal end by reductive coupling using lactose and sodium cyanoborohydride. A synthesis method of conjugating poly(L-lysine) (PLL) derivatives with terminally galactose-graft-PEG was developed using ring-opening polymerization of N(ε)-benzyloxycarbonyl-L-lysine-N(α)-carboxyan-hydride (Z-Lys-NCA) initiated onto galactose graft amine-terminated PEG (galactose-PEG-NH2) as a macro-initiator. The synthesis was characterized with ¹H-, ¹³C-NMR, IR and UV spectroscopy, and all of them successfully verified the formation of the co-polymers. The gel-retardation assay of the complexes between galactose-PEG-PLL and plasmid DNA indicated that these polymeric gene carriers demonstrated the potent ability to condense plasmid DNA electrostatically as well as PLL. The particle size and zeta potential of polymer/DNA complexes were measured, and their cytotoxicity and transfection efficiency in different cells were evaluated. The results indicate that galactose-PEG-PLL can form a complex with plasmid DNA and serve as an effective gene-delivery carrier with lower cytotoxicity compared to that of PLL. Transfection experiments clearly showed that galactose-PEG-PLL effectively delivered DNA into hepatoma cells in vitro. Such data demonstrates that galactose and its complex with plasmid DNA may serve as a safe and effective gene-transfer system targeting hepatocytes.


Subject(s)
Drug Carriers/chemistry , Drug Carriers/metabolism , Galactose/chemistry , Hepatocytes/metabolism , Polyethylene Glycols/chemistry , Polylysine/chemistry , Transfection/methods , Amines/chemistry , Cell Line , DNA/chemistry , DNA/metabolism , Deoxyribonuclease I/metabolism , Drug Carriers/chemical synthesis , Drug Carriers/toxicity , Electrophoresis, Agar Gel , Humans , Hydrophobic and Hydrophilic Interactions , Ligands
4.
Yao Xue Xue Bao ; 46(1): 102-8, 2011 Jan.
Article in Chinese | MEDLINE | ID: mdl-21465815

ABSTRACT

Polyamidoamine-polyethylene glycol (PAMAM-PEG) copolymers were synthesized using IPDI as coupling reagent by two-step method. The copolymers were characterized by IR spectrum and 1H NMR spectrum, and the PEG conjugating ratios of the copolymers were calculated equal to 10% and 30% separately. MTT assay indicated that after PEGylation a lower cytotoxicity of the copolymers could be found, and with increasing PEG conjugating ratio the cytotoxicity decreased obviously. Agarose gel retardation assay demonstrated that PAMAM-PEG copolymers could be combined with DNA and PAMAM-PEG/DNA complexes were prepared by self-assembly. DLS measurement showed that when N/P > or = 50, the particle size of copolymer/ gene complexes was in a range of 150-200 nm, and the zeta potential was in a range of 10-25 mV. In vitro gene transfection illustrated that when N/P < or = 50, the gene transfection efficiency of PAMAM-PEG copolymers was a little less than that of PAMAM-G5, but the transfection efficiency can be raised by increasing N/P ratio or transfection time. Considering both cytotoxicity and transfection efficiency aspects PAMAM-PEG-13 was more effect than PAMAM-PEG-39 in PEGylation.


Subject(s)
Cell Survival/drug effects , DNA/chemistry , Dendrimers/chemical synthesis , Genetic Vectors , Polyethylene Glycols/chemical synthesis , Carcinoma, Hepatocellular/pathology , Cell Line, Tumor , DNA/pharmacology , Dendrimers/pharmacology , Gene Transfer Techniques , Humans , Isocyanates/chemistry , Liver Neoplasms/pathology , Particle Size , Polyamines/chemistry , Polyethylene Glycols/chemistry , Polyethylene Glycols/pharmacology , Transfection
5.
Biomed Mater ; 5(5): 054116, 2010 Oct.
Article in English | MEDLINE | ID: mdl-20876960

ABSTRACT

In this paper, the adsorption behavior of plasma proteins on the surface of ZnO thin films prepared by radio frequency (RF) sputtering under different sputtering powers was studied. The microstructures and surface properties of the ZnO thin films were investigated by x-ray diffraction (XRD), scanning electron microscopy (SEM), UV-visible optical absorption spectroscopy and contact angle techniques. The results show that the ZnO thin films have better orientation of the (0 0 2) peak with increasing RF power, especially at around 160 W, and the optical band gap of the ZnO films varies from 3.2 to 3.4 eV. The contact angle test carried out by the sessile drop technique denoted a hydrophobic surface of the ZnO films, and the surface energy and adhesive work of the ZnO thin films decreased with increasing sputtering power. The amounts of human fibrinogen (HFG) and human serum albumin (HSA) adsorbing on the ZnO films and reference samples were determined by using enzyme-linked immunosorbent assay (ELISA). The results show that fewer plasma proteins and a smaller HFG/HSA ratio adsorb on the ZnO thin films' surface.


Subject(s)
Blood Proteins/pharmacokinetics , Wettability , Zinc Oxide/chemistry , Adsorption , Enzyme-Linked Immunosorbent Assay , Fibrinogen/pharmacokinetics , Humans , Microscopy, Electron, Scanning/methods , Radio Waves , Serum Albumin/pharmacokinetics , Spectrophotometry, Ultraviolet , Surface Properties , X-Ray Diffraction/methods
6.
Biomed Mater ; 4(5): 055004, 2009 Oct.
Article in English | MEDLINE | ID: mdl-19776492

ABSTRACT

ZnO films were first deposited on silicon and glass substrates using radio frequency sputtering and then annealed in air at different temperatures from 300 to 700 degrees C. The microstructures, surface energy and optical properties of ZnO films were examined by x-ray diffraction, Raman spectroscopy, contact angle test and UV-visible optical absorption spectroscopy, respectively. Results show that a perfectly oriented ZnO (0 0 2) thin film is obtained in all ZnO samples. Raman spectroscopy, in combination with those derived by UV-visible optical absorption spectroscopy, provides us with an accurate description of ZnO nature, revealing that, after annealing, ZnO films exhibit better crystallinity and narrower optical energy gap. The contact angle test denotes that the adhesive work and polar component of the surface energy of ZnO films increase steadily with the annealing temperature, which leads to more active interaction between annealed ZnO films and blood plasma. The platelet adhesion experiment shows that there are fewer platelets adhered to the surface of ZnO films compared to the polyurethane (PU) used in clinical application, suggesting ZnO's better compatibility with blood. As the annealing temperature increases, the number of platelets adhered to ZnO films increases correspondingly, which we believe is due to the narrower optical energy gap. Therefore, the appropriate surface properties and the wide optical energy gap of ZnO thin films are believed to be the main factors responsible for the excellent haemocompatibility.


Subject(s)
Biocompatible Materials/chemistry , Blood Platelets/cytology , Blood Platelets/physiology , Membranes, Artificial , Platelet Adhesiveness/physiology , Zinc Oxide/chemistry , Zinc Oxide/radiation effects , Cell Survival , Cells, Cultured , Crystallization/methods , Hot Temperature , Humans , Materials Testing , Particle Size , Radio Waves , Surface Properties
7.
Yao Xue Xue Bao ; 43(8): 848-54, 2008 Aug.
Article in Chinese | MEDLINE | ID: mdl-18956779

ABSTRACT

Chitosan and its derivatives are extensively studied as non-viral gene delivery vectors nowadays. Polyethylene glycol-chitosan (mPEG-CS) copolymers were synthesized by oxidation of mPEG-OH and then combined mPEG-CHO with amino groups on chitosan chains. The in vitro cytotoxicity of copolymers was evaluated by MTT method. The results showed > 70% cell viability of HeLa and A549 cells after incubation with mPEG-CS copolymer from concentration 5 to 100 microg x mL(-1). The mPEG-CS copolymers with various degrees of PEG substitution were combined with DNA and the properties of mPEG-CS/DNA complexes were investigated such as nanoparticle size, zeta potential and agarose gel analysis. The best one among all these mPEG-CS copolymers was mPEG (3.55) -CS, for its capability to condense plasmid DNA was most efficient. For this reason, mPEG (3.55) -CS was picked out to mediate plasmid enhanced green fluorescence protein (pEGFP) and transfect HeLa and A549 cells. The expression of green fluorescence protein was observed by fluorescence microscope and the transfection efficiency was detected by flow cytometry. The gene expression mediated by mPEG-CS was resistant to serum, and the optimal transfection efficiency (8.1% for HeLa cells and 4.8% for A549 cells) of mPEG-CS/EGFP system was obtained under the condition of N/P 40 and 48 h transfection time. These results indicate that mPEG-CS copolymer is an efficient non-viral gene vector.


Subject(s)
Chitosan/chemistry , Genetic Vectors/chemistry , Polyethylene Glycols/chemistry , Transfection , Adenocarcinoma/pathology , Cell Line, Tumor , Chitosan/toxicity , Drug Carriers , HeLa Cells , Humans , Lung Neoplasms/pathology , Nanoparticles , Particle Size , Plasmids , Polyethylene Glycols/toxicity , Polymers
8.
Yao Xue Xue Bao ; 43(4): 408-14, 2008 Apr.
Article in Chinese | MEDLINE | ID: mdl-18664205

ABSTRACT

Polyethylene glycol-polybenzyl-L-glutamate copolymer (PEG-PBLG) was synthesized and paclitaxel-loaded core-shell type nano-micelles with amphiphilic copolymer PEG-PBLG was prepared by the dialysis method. The drug loading content and entrapment efficiency were determined by HPLC. The average size and its distribution were determined by dynamic light scattering method. The paclitaxel release rate in vitro from micelles was measured by HPLC. The cell cytotoxicity in vitro was observed with MTT assay. The anti-tumor activity of paclitaxel-loaded micelles were evaluated in tumor-inhibiting test of nude mice using human liver cancer HepG-2. The results indicated that paclitaxel could be entrapped in PEG-PBLG copolymer micelles and its size was in the range of 80-265 nm which increased with an increase in molecular weight of PBLG in copolymer; in vitro the paclitaxel could be released sustainably from the micelles. In high concentration of paclitaxel (>20 microg x mL(-1)) the paclitaxel-loaded PEG-PBLG micelles displayed much less cell cytotoxicity than paclitaxel injections with Cremophor EL (P<0.05); the tumor inhibiting activity of paclitaxel-loaded PEG-PBLG micelles was similar to that of paclitaxel injections with Cremophor EL in the same paclitaxel concentration. It was concluded that the paclitaxel-loaded PEG-PBLG micelles had more uniform size and size distribution, excellent drug sustainable-release behavior, less cytotoxicity, good anti-tumor activity similar to paclitaxel injections with Cremophor EL. So paclitaxel-loaded PEG-PBLG micelles would be a novel paclitaxel preparation in clinic for the treatment of tumor.


Subject(s)
Drug Delivery Systems , Liver Neoplasms, Experimental/pathology , Paclitaxel/pharmacology , Animals , Antineoplastic Agents, Phytogenic/pharmacology , Cell Line, Tumor , Delayed-Action Preparations , Humans , Mice , Mice, Inbred BALB C , Mice, Nude , Micelles , Nanoparticles , Neoplasm Transplantation , Particle Size , Polyethylene Glycols/chemistry , Polyglutamic Acid/analogs & derivatives , Polyglutamic Acid/chemistry , Polymers , Random Allocation
9.
J Biomed Mater Res A ; 84(3): 795-804, 2008 Mar 01.
Article in English | MEDLINE | ID: mdl-17635020

ABSTRACT

An ideal gene carrier is required both in safety and efficiency for transfection. Polyethylenimine (PEI), a well-studied cationic polymer, has been proved with high transfection efficiency, but is reported as toxicity in many cell lines. In this study, PEI was coupled with polyethylene glycol (PEG) to reduce its cytotoxicity. PEG-PEI copolymers were synthesized with isoporon diisocyanate (IPDI) in two steps. A set of PEG-PEI with different PEG molecular weights (MWs) and amounts of PEG were synthesized. The molecular structure of the resulting copolymers was evaluated by nuclear magnetic resonance spectroscopy ((1)H NMR), infrared spectroscopy (IR), and gel permeation chromatography (GPC), all of which had successfully verified formation of the copolymers. The particle size and zeta potential of polymer/DNA complexes were measured, and their cytotoxicity and transfection efficiency in Hela cells were evaluated. We found that the copolymer block structure significantly influenced not only the physicochemical properties of complexes, but also their cytotoxicity and transfection efficiency. PEG (5 kDa) significantly reduced the diameter of the spherical complexes. The zeta potential of complexes was reduced with increasing amount of PEG grafting. Cytotoxicity was dependent not on PEG MW but on the amount of PEG grafting. Copolymer PEG-PEI (2-25-1) with 1.89 PEG (2 kDa) was proved to be more efficient for in vitro gene transfer. In conclusion, PEG MW and the degree of PEGylation were found to significantly influence the biological activity of PEG-PEI/DNA complexes. These results provide new sights into the studies using block copolymer as gene delivery systems.


Subject(s)
Gene Transfer Techniques , Genetic Vectors , Polyethylene Glycols , Polyethyleneimine , Genetic Therapy , Genetic Vectors/chemical synthesis , Genetic Vectors/chemistry , HeLa Cells , Humans , Molecular Weight , Polyethylene Glycols/chemistry , Polyethyleneimine/chemistry , Spectrophotometry, Infrared
10.
J Biomater Appl ; 22(2): 181-92, 2007 Sep.
Article in English | MEDLINE | ID: mdl-17255156

ABSTRACT

Polybenzyl glutamate (PBLG) or polymethyl glutamate (PMLG) films have been aminolyzed with amino alcohol and crosslinked with aliphatic diamine at 60 degrees C for 48 h simultaneously which led to the formation of crosslinked films of polyhydroxyalkyl glutamine (PHAG). ATR-IR indicates that for the aminolysis of PBLG with 2-amino-1-ethanol or 3-amino-1-propanol, benzyl glutamate almost completely turned to hydroxyalkyl glutamine, however for the aminolysis of PMLG with 5-amino-1-pentanol, methyl glutamate partially turned to hydroxypentanyl glutamine. The water-swelling test shows that water-swelling ratio Q of PHAG films from amino alcohol with longer carbon chain was smaller, the PHAG films crosslinked by 1,2-diamino ethane have the higher water-swelling ratio Q, but the PHAG films crosslinked by 1,8-diamino octane have the lower water swelling ratio Q; and PHAG films with a greater amount of crosslinking agents have high crosslinking density or the low water swelling-ratio Q for same amino alcohol and diamine. It is obvious from in vitro enzymatic hydrolysis test that specimens with smaller swelling ratio Q displayed larger T(1/2), time for half weight digestion of PHAG film, that is, less biodegradability. Therefore, biodegradability of the crosslinked PHAG films can be controlled by changing amino alcohol and diamine.


Subject(s)
Amino Alcohols/chemistry , Biocompatible Materials/chemistry , Diamines/chemistry , Polyglutamic Acid/analogs & derivatives , Biocompatible Materials/chemical synthesis , Cross-Linking Reagents/chemistry , Hydrolysis , Materials Testing , Papain/chemistry , Polyglutamic Acid/chemical synthesis , Polyglutamic Acid/chemistry , Spectrophotometry, Infrared
11.
Cardiology ; 106(2): 82-8, 2006.
Article in English | MEDLINE | ID: mdl-16612074

ABSTRACT

The increases in physiological levels of fluid shear stress have beneficial effects on vascular homeostasis. Endothelial progenitor cells (EPCs) play an important role in the maintenance of endothelial integrity. We hypothesized that shear stress-mediated vascular protection is related to the upregulation of endothelial nitric oxide synthase expression in EPCs. The human EPCs exposed to in vitro shear stress levels of 5, 15 and 25 dyn/cm(2) for 4 h. In vitro shear stress, in a dose-dependent fashion, increased the endothelial nitric oxide synthase mRNA expression and the nitric oxide production in human EPCs. The present findings for the first time provide novel insights into the mechanisms of the physiological levels of fluid shear stress on the regulation of human EPC biologic phenotype as a potential factor, which might contribute to vascular protective activities in humans although evidence is indirect.


Subject(s)
Adult Stem Cells/metabolism , Nitric Oxide Synthase Type III/metabolism , Cells, Cultured , Endothelial Cells/metabolism , Gene Expression , Humans , Nitrogen Oxides/metabolism , RNA, Messenger/metabolism , Stress, Mechanical
12.
Biochem Biophys Res Commun ; 342(2): 577-84, 2006 Apr 07.
Article in English | MEDLINE | ID: mdl-16488398

ABSTRACT

Seeding endothelial progenitor cells (EPCs) onto the surface of vascular grafts has been proved to be a promising strategy to improve nonthrombogenic potentials of small diameter artificial vessels. Here, we investigated whether in vitro shear stress modulates the tissue-type plasminogen activator (t-PA) secretion and mRNA expression in human EPCs and improves patency of the EPC-seeded polyurethane small diameter vascular grafts implanted in the canine carotid artery in vivo. In vitro shear stress, in a dose-dependent manner, increased t-PA secretion and mRNA expression of human EPCs. The in vivo implantation of EPC-seeded vascular grafts remained highly patent in shear stress pretreatment compared with stationary condition. The present findings demonstrate for the first time that in vitro shear stress can enhance t-PA secretion and gene expression in human EPCs, which contributes to improvement in nonthrombogenic potentials of EPC-seeded small diameter artificial vessels with maintenance of in vivo highly patency rate.


Subject(s)
Blood Vessel Prosthesis Implantation , Endothelial Cells/metabolism , RNA, Messenger/biosynthesis , Stem Cells/metabolism , Tissue Plasminogen Activator/biosynthesis , Tissue Plasminogen Activator/genetics , Vascular Patency/physiology , Animals , Blood Flow Velocity , Carotid Artery, Common/transplantation , Cells, Cultured , Dogs , Endothelial Cells/transplantation , Endothelial Cells/ultrastructure , Humans , Male , Microscopy, Fluorescence , Microscopy, Phase-Contrast , Stem Cell Transplantation , Stem Cells/ultrastructure , Tissue Plasminogen Activator/metabolism , Up-Regulation/genetics , Vascular Patency/genetics
13.
Zhonghua Xin Xue Guan Bing Za Zhi ; 33(9): 840-2, 2005 Sep.
Article in Chinese | MEDLINE | ID: mdl-16266463

ABSTRACT

OBJECTIVE: In order to investigate the role of shear stress in the regulation of endothelial function, we assessed here effects of shear stress on tissue-type plasminogen activator in human endothelial progenitor cells (EPCs). METHODS: The peripheral blood mononuclear cells were separated from healthy adult and inducted into EPCs, which were identified by double staining for the fluorescent labeled acetylated-LDL and lectin. EPCs were seeded on the small diameter artificial vessels, and then divided into four different experimental groups including stationary group, low-flow shear stress group (5 dyn/cm(2)), medium-flow shear stress group (15 dyn/cm(2)) and high-flow shear stress group (25 dyn/cm(2)). The levels of t-PA in EPC culture medium at 0 hour, 5 hours, 10 hours, 15 hours, 20 hours and 25 hours after culture were measured by enzyme-linked immunosorbent assay. RESULTS: The peripheral blood mononuclear cells differentiated into EPCs after induction, which were positively labeled by fluorescent acetylated-LDL and lectin. Shear stress enhanced production of the t-PA by EPCs, which was paralleled to levels and times of shear stress. CONCLUSIONS: Shear stress increases t-PA secretion by human EPCs, suggesting that shear stress not only regulates vascular endothelial function but also participates in the pathogenesis of arteriosclerosis.


Subject(s)
Endothelial Cells/metabolism , Stem Cells/metabolism , Stress, Mechanical , Tissue Plasminogen Activator/metabolism , Adult , Humans
14.
Ai Zheng ; 23(4): 381-5, 2004 Apr.
Article in Chinese | MEDLINE | ID: mdl-15087023

ABSTRACT

BACKGROUND & OBJECTIVE: 5-Fluorouracil (5-FU) belongs to antimetabolic anticancer drugs and its half-life time in vivo is only about 5 minutes. Continuous infusion (48 hours,72 hours,28 days) was commonly used to maintain long-time steady-state concentration (Css). So it is necessary to exploit new slow-release system for 5-FU. This article was designed to investigate the preparation technique,shape characteristics, and drug releasing characteristics in vivo of 5-FU loaded core-shell type nanoparticles which were made by biodegradable amphiphlic poly (ethylene glycol)-poly (gamma-benzyl-L-glutamate)(PEG-PBLG). METHODS: The PEG-PBLG nano-micelles were prepared by diafiltration method. Its morphology was observed by transmission electron microscopy and scan electron microscopy. Encapsulating efficiency of 5-FU was determined by ultraviolet spectrophotometry. The 5-FU releasing characteristics from nano-micelles in vivo were investigated by high-performance liquid chromatography (HPLC). RESULTS: 5-FU loaded PEG-PBLG copolymer nano-micelles (5-FU/PEG-PBLG) was of round or ellipsic shape. The diameter of the micelles was 180-250 nm; the size of drug storeroom was about 200 nm and the thickness of hydrophilic zone was about 30 nm. The entrapment efficiency was (29.5+/-0.015)%. In control group, 5-FU is one-compartment in vivo; its half-life was 5.3 minutes; the maximum plasma concentration (C(max)) was 17047.3 microg/L; T(max) was the time of attaining C(max) of the end of infusion; the area under the plasma concentration-time curve (AUC) was 6263.7 microg/L x min. However, the model of nano-micelles in vivo was typical release-drug of nano-micelles namely abrupt release-slow release; its t(1/2) was 63.2 minutes; C(max) was 4563.5 microg/L; T(max) was 1.25 hours; AUC was 5794.5 microg/Lxmin. Compared with 5-FU preparation, T(max) of 5-FU/PEG-PBLG was longer (P< 0.01);C(max) was lower (P< 0.01);t(1/2) was longer (P< 0.01); AUC was similar (P >0.01). CONCLUSION: The 5-FU/PEG-PBLG nano-micelles can change the pharmacokinetics of 5-FU, prolonging the circulation time in vivo and make a slow release.


Subject(s)
Fluorouracil/administration & dosage , Polyethylene Glycols/administration & dosage , Polyglutamic Acid/analogs & derivatives , Polyglutamic Acid/administration & dosage , Animals , Area Under Curve , Fluorouracil/pharmacokinetics , Male , Micelles , Molecular Weight , Rabbits
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