Dendrimer-like amphiphilic copolymer is a kind of three-dimensional spherical structure polymer. An amphiphilic dendrimer-like diblock copolymer, PEEGE-G2-b-PEO(OH)12, constituted of a hydrophobic poly(ethoxyethyl ...Dendrimer-like amphiphilic copolymer is a kind of three-dimensional spherical structure polymer. An amphiphilic dendrimer-like diblock copolymer, PEEGE-G2-b-PEO(OH)12, constituted of a hydrophobic poly(ethoxyethyl glycidol ether) inner core and a hydrophilic poly(ethylene oxide) outer layer, has been successfully synthesized by the living anionic ring-opening polymerization method. The intermediates and targeted products were charac-terized with 1H NMR spectroscopy and gel permeation chromatography. The application on drug delivery of dendrimer-like diblock copolymer PEEGE-G2-b-PEO(OH)12 using DOX as a model drug was also studied. The drug loading content and encapsulation e ciency were found at 13.07% and 45.75%, respectively. In vitro release experiment results indicated that the drug-loaded micelles exhibited a sustained release behavior under acidic media.展开更多
Novel pH-responsive membranes were prepared by blending pH-responsive amphiphilic copolymers with polyethersulfone(PES) via a nonsolvent-induced phase separation(NIPS) technique. The amphiphilic copolymers bearing Plu...Novel pH-responsive membranes were prepared by blending pH-responsive amphiphilic copolymers with polyethersulfone(PES) via a nonsolvent-induced phase separation(NIPS) technique. The amphiphilic copolymers bearing Pluronic F127 and poly(methacrylic acid)(PMAA) segments, abbreviated as PMAA n–F127–PMAA n,were synthesized by free radical polymerization. The physical and chemical properties of the blend membranes were evaluated by scanning electron microscopy(SEM), Fourier transform infrared(FTIR) spectrum, water contact angle, Zeta potential and X-ray photoelectron spectroscopy(XPS). The enrichment of hydrophilic PMAA segments on the membrane surfaces was attributed to surface segregation during the membrane preparation process. The blend membranes had signi ficant p H-responsive properties due to the conformational changes of surface-segregated PMAA segments under different pH values of feed solutions. Fluxes of the blend membranes were larger at low p H values of feed solutions than that at high pH values. The pH-responsive ability of the membranes was enhanced with the increase of the degree of PMAA near-surface coverage.展开更多
The objective of the work involves the synthesis of comb-like amphiphilic cationic polymers with repeating units methacylamides laterally substituted by a group containing a quaternary ammonium site and a hydrophobic ...The objective of the work involves the synthesis of comb-like amphiphilic cationic polymers with repeating units methacylamides laterally substituted by a group containing a quaternary ammonium site and a hydrophobic n-alkyl side chain with 8-10 carbon atoms. Two synthesis methods were developed successfully. The first method is consisted to synthesizing first amphiphilic cationic methacrylamide monomers. In the second method the tertiary amine groups of polymers precursors were quaternised with various n-alkyl bromides. All the polymers obtained in this way were characterized by spectroscopic methods: 1^H NMR and by viscometry. The reduced viscosity of hydro-alcoholic polymer solution decreases with polymer concentration. Viscometry study showed that these polymers display typical polysoap behavior in hydro-alcoholic mixtures.展开更多
An amphiphilic polymer bearing tetraphenylethene (TPE) moiety was synthesized by convenient reactions. The polymer exhibits unique aggregation-induced emission (AIE) characteristics and can self-assemble to size-tunab...An amphiphilic polymer bearing tetraphenylethene (TPE) moiety was synthesized by convenient reactions. The polymer exhibits unique aggregation-induced emission (AIE) characteristics and can self-assemble to size-tunable particles in DMF/water mixtures. The polymer nanoparticles can be used for cell imaging, which provides a potential stable fluorescent tool to monitor the distribution of drugs and bioconjugates in living cells.展开更多
Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles(NPs) by a dou...Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles(NPs) by a double emulsion-solvent evaporation(DESE) method. The particle size and drug encapsulation efficacy(EE) were compared to evaluate and optimize the preparation parameters. The mixed NPs had average size ranging from(102±1) nm to(137±5) nm, and the zeta potential turned to positive with incorporation of the amphiphilic dendrimer. The NPs showed different EE of docetaxel(DTX) and paclitaxel(PTX) with higher affinity to more lipophilic PTX. The blank mixed NPs showed little cytotoxicity, and the DTX-loaded NPs could effectively facilitate the antiproliferation activity on PC-3 cells. The NPs could be used as an effective drug delivery system, and its anti-tumor effect is worthy of further study.展开更多
In the past few years there has been a growth in the use of nanoparticles for stabilizing lipid membranes that contain embedded proteins. These bionanoparticles provide a solution to the challenging problem of membran...In the past few years there has been a growth in the use of nanoparticles for stabilizing lipid membranes that contain embedded proteins. These bionanoparticles provide a solution to the challenging problem of membrane protein isolation by maintaining a lipid bilayer essential to protein integrity and activity. We have previously described the use of an amphipathic polymer (poly(styrene-co-maleic add), SMA) to produce discoidal nanoparticles with a lipid bilayer core containing the embedded protein. However the structure of the nanoparticle itself has not yet been determined. This leaves a major gap in understanding how the SMA stabilizes the encapsulated bilayer and how the bilayer relates physically and structurally to an unencapsulated lipid bilayer. In this paper we address this issue by describing the structure of the SMA lipid particle (SMALP) using data from small angle neutron scattering (SANS), electron microscopy (EM), attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and nuclear magnetic resonance spectroscopy (NMR). We show that the particle is disc shaped containing a polymer "bracelet" encircling the lipid bilayer. The structure and orientation of the individual components within the bilayer and polymer are determined showing that styrene moieties within SMA intercalate between the lipid acyl chains. The dimensions of the encapsulated bilayer are also determined and match those measured for a natural membrane. Taken together, the description of the structure of the SMALP forms the foundation for future development and applications of SMALPs in membrane protein production and analysis.展开更多
The use of nanotechnology in drug-delivery systems(DDS) is attractive for advanced diagnosis and treatment of cancer diseases. Biodegradable polymeric nanoparticles, for example, have promising applications as advance...The use of nanotechnology in drug-delivery systems(DDS) is attractive for advanced diagnosis and treatment of cancer diseases. Biodegradable polymeric nanoparticles, for example, have promising applications as advanced drug carriers in cancer treatment. In this review, we discuss the development of drug-delivery systems based on an amphiphilic principle mainly conducted by our group for anti-cancer drug delivery. We first briefly address the synthetic chemistry for amphiphilic biodegradable polymers. In the second part, we summarize progress in the application of self-assembled polymer micelles using amphiphilic biodegradable copolymers as anti-tumor drug carriers.展开更多
Synthetic polymer membranes are widely used in many applications,including,among others,water purification,protein separation,and medicine.However,the use of existing polymer membranes faces major challenges,such as t...Synthetic polymer membranes are widely used in many applications,including,among others,water purification,protein separation,and medicine.However,the use of existing polymer membranes faces major challenges,such as the trade-off between permeability and selectivity,membrane fouling,and poor mechanical strength.To address these problems the authors have focused their research on surface/interfacial tailoring and the structure-property relationship of polymer membranes used in liquid separation systems.Progress has been made as follows:(1)a methodology for membrane surface functionalization and nanofiltration(NF)membrane preparation based on mussel-inspired catecholic chemistry was proposed and established;(2)a class of mechanically robust and environmentally-responsive composite membranes with hydrogel pore-filled in rigid macroporous supports was designed and developed;(3)a methodology for surface tailoring and antifouling modification of polymer membranes based on amphiphilic copolymers was created and the scientific implications for amphiphilic polymer membranes elaborated;(4)an adsorption membrane with both filtration and adsorption functions was designed and developed to achieve rapid removal of trace micropollutants,including heavy metal ions,organic dyes,plasticizer,antibiotics,and others.This mini-review briefly summarizes this work.展开更多
In the present study, we aimed to explore the structure-activity relationship for the new amphiphilic material rhamnoside with antibacterial biofilm activity, and provide the basis for selecting rhamnoside with the op...In the present study, we aimed to explore the structure-activity relationship for the new amphiphilic material rhamnoside with antibacterial biofilm activity, and provide the basis for selecting rhamnoside with the optimum antibacterial biofilm activity. A series of alkyl rhamnosides with different carbon chain lengths were obtained by a simple and effective synthesis method. The structure was characterized by ~1H NMR spectrum, and their critical micelle concentration(CMC) was measured by fluorescence probe method. The hydrophilic and lipophilic balance(HLB) value was obtained by calculation. The minimal inhibitory concentration(MIC) of Staphylococcus aureus was determined by the broth double dilution method. The effect of biofilm inhibition and biofilm disruption was assayed by crystal violet method. The results showed that with the increase of carbon chain length, the CMC and HLB of alkyl rhamnosides displayed a linear downward trend, indicating that the lipophilicity and surface activity of the alkyl rhamnoside were increased. At the same time, the antibacterial activity in vitro produced the maximum, ie, 12-hydroxydecanoyl rhamnoside had the strongest antibacterial activity in vitro. Similarly, this material also exhibited the strongest antibacterial biofilm activity in vitro. The results of this study demonstrated that the most potent active material was obtained through the structure-activity relationship and it could be applied antibacterial biofilms in clinical practice.展开更多
Amphiphilic graft copolymers are excellent additives for the development of antifouling membranes by nonsolvent induced phase separation. We report a convenient approach to the synthesis of novel graft copolymers with...Amphiphilic graft copolymers are excellent additives for the development of antifouling membranes by nonsolvent induced phase separation. We report a convenient approach to the synthesis of novel graft copolymers with hydrophobic polyacryloni- trile (PAN) backbones and hydrophilic poly(2-hydroxyethyl methacrylate) (PHEMA) side chains. Atom transfer radical polymerization (ATRP) of 2-hydroxyethyl methacrylate was carried out with poly(acrylonitrile-co-p-chloromethyl styrene) (PAN-co-PCMS) as a macroinitiator in the presence of CuC1/2,2'-bipyridine at 50 ~C in dimethyl sulfoxide. Kinetics of the graft polymerization was also evaluated. The synthesis of poly(acrylonitrile-co-p-chloromethyl styrene-g-2-hydroxyethyl methacrylate) (PAN-co-(PCMS-g-PHEMA)) can be relatively controlled when CMS (the ATRP sites) unit in the macroinitia- tor is around 5 mol%. Both the macroinitiators and graft copolymers were characterized by FTIR, NMR and GPC. The surface morphology and wettability of the copolymer films were studied by AFM and water contact angle measurement, respectively. We demonstrate that phase segregation between the PAN-co-PCMS backbones and the PHEMA side chains takes place and the surface hydrophilicity of the graft copolymers increases with the length of the PHEMA side chains. Because these am- phiphilic graft copolymers can be synthesized in mass, they will be useful as latent additives for the fabrication of advanced PAN separation membranes.展开更多
文摘Dendrimer-like amphiphilic copolymer is a kind of three-dimensional spherical structure polymer. An amphiphilic dendrimer-like diblock copolymer, PEEGE-G2-b-PEO(OH)12, constituted of a hydrophobic poly(ethoxyethyl glycidol ether) inner core and a hydrophilic poly(ethylene oxide) outer layer, has been successfully synthesized by the living anionic ring-opening polymerization method. The intermediates and targeted products were charac-terized with 1H NMR spectroscopy and gel permeation chromatography. The application on drug delivery of dendrimer-like diblock copolymer PEEGE-G2-b-PEO(OH)12 using DOX as a model drug was also studied. The drug loading content and encapsulation e ciency were found at 13.07% and 45.75%, respectively. In vitro release experiment results indicated that the drug-loaded micelles exhibited a sustained release behavior under acidic media.
基金Supported by the National Natural Science Foundation for Distinguished Young Scholars(No.21125627)the Natural Science Foundation of Tianjin(Nos.13JCYBJC20500,14JCZDJC37400)
文摘Novel pH-responsive membranes were prepared by blending pH-responsive amphiphilic copolymers with polyethersulfone(PES) via a nonsolvent-induced phase separation(NIPS) technique. The amphiphilic copolymers bearing Pluronic F127 and poly(methacrylic acid)(PMAA) segments, abbreviated as PMAA n–F127–PMAA n,were synthesized by free radical polymerization. The physical and chemical properties of the blend membranes were evaluated by scanning electron microscopy(SEM), Fourier transform infrared(FTIR) spectrum, water contact angle, Zeta potential and X-ray photoelectron spectroscopy(XPS). The enrichment of hydrophilic PMAA segments on the membrane surfaces was attributed to surface segregation during the membrane preparation process. The blend membranes had signi ficant p H-responsive properties due to the conformational changes of surface-segregated PMAA segments under different pH values of feed solutions. Fluxes of the blend membranes were larger at low p H values of feed solutions than that at high pH values. The pH-responsive ability of the membranes was enhanced with the increase of the degree of PMAA near-surface coverage.
文摘The objective of the work involves the synthesis of comb-like amphiphilic cationic polymers with repeating units methacylamides laterally substituted by a group containing a quaternary ammonium site and a hydrophobic n-alkyl side chain with 8-10 carbon atoms. Two synthesis methods were developed successfully. The first method is consisted to synthesizing first amphiphilic cationic methacrylamide monomers. In the second method the tertiary amine groups of polymers precursors were quaternised with various n-alkyl bromides. All the polymers obtained in this way were characterized by spectroscopic methods: 1^H NMR and by viscometry. The reduced viscosity of hydro-alcoholic polymer solution decreases with polymer concentration. Viscometry study showed that these polymers display typical polysoap behavior in hydro-alcoholic mixtures.
基金supported by the National Natural Science Foundation of China (20974028, 20974098, and 21174120)the National Basic Research Program of China (2009CB623605)+1 种基金the Research Grants Council of Hong Kong (603509, HKUST2/CRF/10, 604711, and N_HKUST620/11)B.Z.T. thanks the support from the Cao Guangbiao Foundation of Zhejiang University
文摘An amphiphilic polymer bearing tetraphenylethene (TPE) moiety was synthesized by convenient reactions. The polymer exhibits unique aggregation-induced emission (AIE) characteristics and can self-assemble to size-tunable particles in DMF/water mixtures. The polymer nanoparticles can be used for cell imaging, which provides a potential stable fluorescent tool to monitor the distribution of drugs and bioconjugates in living cells.
基金National Natural Science Foundation of China(Grant No.81473156,81673365,81273454)Doctoral Foundation of the Ministry of Education(Grant No.20130001110055)National Key Basic Research Program(Grant No.2013CB932501)
文摘Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles(NPs) by a double emulsion-solvent evaporation(DESE) method. The particle size and drug encapsulation efficacy(EE) were compared to evaluate and optimize the preparation parameters. The mixed NPs had average size ranging from(102±1) nm to(137±5) nm, and the zeta potential turned to positive with incorporation of the amphiphilic dendrimer. The NPs showed different EE of docetaxel(DTX) and paclitaxel(PTX) with higher affinity to more lipophilic PTX. The blank mixed NPs showed little cytotoxicity, and the DTX-loaded NPs could effectively facilitate the antiproliferation activity on PC-3 cells. The NPs could be used as an effective drug delivery system, and its anti-tumor effect is worthy of further study.
文摘In the past few years there has been a growth in the use of nanoparticles for stabilizing lipid membranes that contain embedded proteins. These bionanoparticles provide a solution to the challenging problem of membrane protein isolation by maintaining a lipid bilayer essential to protein integrity and activity. We have previously described the use of an amphipathic polymer (poly(styrene-co-maleic add), SMA) to produce discoidal nanoparticles with a lipid bilayer core containing the embedded protein. However the structure of the nanoparticle itself has not yet been determined. This leaves a major gap in understanding how the SMA stabilizes the encapsulated bilayer and how the bilayer relates physically and structurally to an unencapsulated lipid bilayer. In this paper we address this issue by describing the structure of the SMA lipid particle (SMALP) using data from small angle neutron scattering (SANS), electron microscopy (EM), attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and nuclear magnetic resonance spectroscopy (NMR). We show that the particle is disc shaped containing a polymer "bracelet" encircling the lipid bilayer. The structure and orientation of the individual components within the bilayer and polymer are determined showing that styrene moieties within SMA intercalate between the lipid acyl chains. The dimensions of the encapsulated bilayer are also determined and match those measured for a natural membrane. Taken together, the description of the structure of the SMALP forms the foundation for future development and applications of SMALPs in membrane protein production and analysis.
基金supported by the National Basic Research Program of China(2011CB606206)the National Natural Science Foundation of China(21372170,51133004 and 81361140343)+1 种基金the Recruitment Program ofGlobal Young Experts of China,the Setup Foundation of Sichuan University(YJ201317)the Excellent Young Teachers Program of SichuanUniversity(2082604164235)
文摘The use of nanotechnology in drug-delivery systems(DDS) is attractive for advanced diagnosis and treatment of cancer diseases. Biodegradable polymeric nanoparticles, for example, have promising applications as advanced drug carriers in cancer treatment. In this review, we discuss the development of drug-delivery systems based on an amphiphilic principle mainly conducted by our group for anti-cancer drug delivery. We first briefly address the synthetic chemistry for amphiphilic biodegradable polymers. In the second part, we summarize progress in the application of self-assembled polymer micelles using amphiphilic biodegradable copolymers as anti-tumor drug carriers.
基金Project supported by the National Natural Science Foundation of China(Nos.51828301,51773175,and 51973185)the Fundamental Research Funds for the Central Universities,China。
文摘Synthetic polymer membranes are widely used in many applications,including,among others,water purification,protein separation,and medicine.However,the use of existing polymer membranes faces major challenges,such as the trade-off between permeability and selectivity,membrane fouling,and poor mechanical strength.To address these problems the authors have focused their research on surface/interfacial tailoring and the structure-property relationship of polymer membranes used in liquid separation systems.Progress has been made as follows:(1)a methodology for membrane surface functionalization and nanofiltration(NF)membrane preparation based on mussel-inspired catecholic chemistry was proposed and established;(2)a class of mechanically robust and environmentally-responsive composite membranes with hydrogel pore-filled in rigid macroporous supports was designed and developed;(3)a methodology for surface tailoring and antifouling modification of polymer membranes based on amphiphilic copolymers was created and the scientific implications for amphiphilic polymer membranes elaborated;(4)an adsorption membrane with both filtration and adsorption functions was designed and developed to achieve rapid removal of trace micropollutants,including heavy metal ions,organic dyes,plasticizer,antibiotics,and others.This mini-review briefly summarizes this work.
基金National Natural Science Foundation of China(Grant No.81573381)CAMS Initiative for Innovative Medicine(Grant No.CAMS-I2M-1-012)
文摘In the present study, we aimed to explore the structure-activity relationship for the new amphiphilic material rhamnoside with antibacterial biofilm activity, and provide the basis for selecting rhamnoside with the optimum antibacterial biofilm activity. A series of alkyl rhamnosides with different carbon chain lengths were obtained by a simple and effective synthesis method. The structure was characterized by ~1H NMR spectrum, and their critical micelle concentration(CMC) was measured by fluorescence probe method. The hydrophilic and lipophilic balance(HLB) value was obtained by calculation. The minimal inhibitory concentration(MIC) of Staphylococcus aureus was determined by the broth double dilution method. The effect of biofilm inhibition and biofilm disruption was assayed by crystal violet method. The results showed that with the increase of carbon chain length, the CMC and HLB of alkyl rhamnosides displayed a linear downward trend, indicating that the lipophilicity and surface activity of the alkyl rhamnoside were increased. At the same time, the antibacterial activity in vitro produced the maximum, ie, 12-hydroxydecanoyl rhamnoside had the strongest antibacterial activity in vitro. Similarly, this material also exhibited the strongest antibacterial biofilm activity in vitro. The results of this study demonstrated that the most potent active material was obtained through the structure-activity relationship and it could be applied antibacterial biofilms in clinical practice.
基金supported by the National Natural Science Foundation of China (21174124)
文摘Amphiphilic graft copolymers are excellent additives for the development of antifouling membranes by nonsolvent induced phase separation. We report a convenient approach to the synthesis of novel graft copolymers with hydrophobic polyacryloni- trile (PAN) backbones and hydrophilic poly(2-hydroxyethyl methacrylate) (PHEMA) side chains. Atom transfer radical polymerization (ATRP) of 2-hydroxyethyl methacrylate was carried out with poly(acrylonitrile-co-p-chloromethyl styrene) (PAN-co-PCMS) as a macroinitiator in the presence of CuC1/2,2'-bipyridine at 50 ~C in dimethyl sulfoxide. Kinetics of the graft polymerization was also evaluated. The synthesis of poly(acrylonitrile-co-p-chloromethyl styrene-g-2-hydroxyethyl methacrylate) (PAN-co-(PCMS-g-PHEMA)) can be relatively controlled when CMS (the ATRP sites) unit in the macroinitia- tor is around 5 mol%. Both the macroinitiators and graft copolymers were characterized by FTIR, NMR and GPC. The surface morphology and wettability of the copolymer films were studied by AFM and water contact angle measurement, respectively. We demonstrate that phase segregation between the PAN-co-PCMS backbones and the PHEMA side chains takes place and the surface hydrophilicity of the graft copolymers increases with the length of the PHEMA side chains. Because these am- phiphilic graft copolymers can be synthesized in mass, they will be useful as latent additives for the fabrication of advanced PAN separation membranes.