• Title/Summary/Keyword: Block copolymers

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Isomeric Folate-Conjugated Polymeric Micelles Bind to Folate Receptors and Display Anticancer Effects

  • Dong, Qing;Xie, Zuo-Xu;Xie, Cao;Lu, Wei-Yue;Zhang, Qian;Li, Xue;Liu, Min
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.17
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    • pp.7363-7369
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    • 2014
  • The present study aimed to prepare and evaluate polymeric micelles conjugated with folic acid through ${\alpha}$- or ${\gamma}$-carboxyl groups for antitumor efficacy. The isomeric block copolymers, ${\alpha}$- and ${\gamma}$-folate-polyethyleneglycol-distearoyl phosphatidylethanolamine (${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE), were produced by solid phase peptide synthesis. Three types of doxorubicin (DOX)-loaded polymeric micelles (MPEG-DSPE-DOX and ${\alpha}$- / ${\gamma}$-Fol-PEG-DSPEDOX micelles) were prepared via the film formation method. Compared with MPEG-DSPE-DOX micelles, the ${\alpha}$- / ${\gamma}$-Fol-PEG-DSPE-DOX micelles presented a higher cellular uptake behavior in the live cell study. Cell viability percentages were 81.8%, 57.3%, 56.6% at 2 hours for MPEG-DSPE-DOX, ${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE-DOX micelles, respectively (p<0.05). Using the KB xenograft tumor model, both ${\alpha}$- and ${\gamma}$-folate-conjugated micelles were found to have better antitumor effects with lower toxicity in comparison with MPEG-DSPE-DOX micelles. No difference in in vivo antitumor efficacy was found between ${\alpha}$- and ${\gamma}$-Fol-PEG-DSPE-DOX micelles. The folate-conjugated micelles might be a potentially useful strategy for tumor targeting of therapeutic agents, whether grafting with folic acid through ${\alpha}$- or ${\gamma}$-carboxyl groups.

Preparation of Water-Resistant Hydrophilic Coating Solutions for PET film (내수성이 우수한 PET 필름용 친수성 코팅액의 제조)

  • Lee, Soo
    • Journal of the Korean Applied Science and Technology
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    • v.31 no.4
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    • pp.584-594
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    • 2014
  • To increase of surface hydrophilicity of polymeric thin films is an important approaching technique for introduction of self-cleaning and/or antifogging properties on the surfaces of those films. In general, hydrophilic surface can be produced by coating non ionic surfactants or by increasing surface energy. Various non-ionic surfactants, such as Tween, Span, and PEG-PPG block copolymers were selected for our experiments, because they are cheap and well soluble in toluene system as well as they contain several reactive hydroxy fuctional groups with coupling agents. Blending conditions influence the PET film surface hydrophilicities. However, the introduction of only these surfactants on the surface of PET films did not show the high durability of hydrophilic properties after washing with water. To improve the durability two types of coupling agents such as epoxide and diisocyanate were adopted. Contact angle of water on hydrophilically coated PET film surface with 6 wt% of isophrone diisocyanate(IPDI) containing coating solution was reached to $8.7^{\circ}$, which was an indirect evidence for very high surface hydrophilicity. A light(500 nm of wavelength) transmittance value of coated PET film was changed only from 87% to 85% with keeping a good transparent property. This film can be usable for self-cleaning film industries.

Synthesis and Characterization of Photosensitizer-conjugated Gold Nanorods for Photodynamic/Photothermal Therapy (광역학적/광열치료 응용을 위한 광증감제가 결합한 골드 나노로드의 합성 및 특성분석)

  • Choi, Jongseon;Kim, So Yeon
    • Applied Chemistry for Engineering
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    • v.27 no.6
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    • pp.599-605
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    • 2016
  • Recently, photodynamic and photothermal therapies have received increasing attention as an effective cancer treatment. In this study, a gold nanorod (AuNR) colloidal solution was synthesized as a hyperthermia agent for photothermal therapy and also modified with photosensitizer (PS) for photodynamic therapy. PEG (polyethylene glycol) and FA (folic acid) ligand were also introduced into AuNR for the long circulation in human body and efficient targeting of cancer cells, respectively and AuNRs were modified with FA-PEG and poly-${\beta}$-benzyl-L-aspartate (PBLA) block copolymers through a 3,4-dihydroxy hydrocinnamic acid (HCA) linker. A series of AuNRs with various aspect ratios were synthesized by controlling the feeding ratio of $AgNO_3$. The physicochemical property and morphology of synthesized AuNR100 and FA-PEG-$P(Asp)_{50}$-HCA-AuNR100 were analyzed by UV-visible spectrophotometer, $^1H$ NMR, XPS measurements, TEM. The surface modified AuNR carrier with biocompatibility could be applied for the effective diagnosis as well tumor phototherapy.

Stabilization and Release Behavior of W1/O/W2-Type Multiple Emulsions Using Various Block Copolymer Emulsifier and Stabilizer (다양한 Block Copolymer를 유화제 및 안정화제로 사용한 W1/O/W2-Type 다중에멀젼의 방출거동 및 안정성)

  • Haw, Jung-Rim;Kim, Cheol-Hun
    • Applied Chemistry for Engineering
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    • v.8 no.4
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    • pp.560-567
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    • 1997
  • A new approach to obtain stable $W_1/O/W_2$ multiple emulsions has been studied ; The basis of the interfacial interaction between a PCL-PEO-PCL triblock copolymer and a lipophilic emulsifier in the dispersed oil phase was examined. $W_1/O/W_2$ multiple emulsions were prepared by the two-step method. Arlacel P-l35 was used as a liphophilic emulsifier and Synperonic PE/F 127 as a hydrophilic one. Eutanol-G was used as an oil phase. NaCl was encapsulated within the multiple emulsion droplets as the internal marker and its release rate studies were carried out. The suability of the multiple emulsions have been assessed by measuring Separation Ratios(%) and microscopic observations. The release of NaCl was significantly reduced in $W_1/O/W_2$ multiple emulsions containing PCL-PEO-PCL triblock copolymer(2k-4k-2k or 6k-4k-6k) in the oil phase. It may be concluded that the copolymer and the emulsifier form effective interfacial complex to enhance stability and to control the release rate. The effective diffusion coefficients of the NaCl were estimated as $2.64{\times}10^{-15}s$and $3.23{\times}10^{-16}gcm^2/s$ for the $W_1/O/W_2$ multiple emulsion containing 1.2 wt % of PCL-PEO-PCL triblock copolymers with compositions of 2k-4k-2k and 6k-4k-2k, respectively. The rate of release decreased with the increase of the initial concentration of NaCl. The results were examined in view of Higuchi mechanism. A kinetic model which is similar to the model for release of dispersed drugs from a polymeric matrix was found to be suitable for the release of NaCl from $W_1/O/W_2$ multiple emulsions.

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Recent research activities on hybrid rocket in Japan

  • Harunori, Nagata
    • Proceedings of the Korean Society of Propulsion Engineers Conference
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    • 2011.04a
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    • pp.1-2
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    • 2011
  • Hybrid rockets have lately attracted attention as a strong candidate of small, low cost, safe and reliable launch vehicles. A significant topic is that the first commercially sponsored space ship, SpaceShipOne vehicle chose a hybrid rocket. The main factors for the choice were safety of operation, system cost, quick turnaround, and thrust termination. In Japan, five universities including Hokkaido University and three private companies organized "Hybrid Rocket Research Group" from 1998 to 2002. Their main purpose was to downsize the cost and scale of rocket experiments. In 2002, UNISEC (University Space Engineering Consortium) and HASTIC (Hokkaido Aerospace Science and Technology Incubation Center) took over the educational and R&D rocket activities respectively and the research group dissolved. In 2008, JAXA/ISAS and eleven universities formed "Hybrid Rocket Research Working Group" as a subcommittee of the Steering Committee for Space Engineering in ISAS. Their goal is to demonstrate technical feasibility of lowcost and high frequency launches of nano/micro satellites into sun-synchronous orbits. Hybrid rockets use a combination of solid and liquid propellants. Usually the fuel is in a solid phase. A serious problem of hybrid rockets is the low regression rate of the solid fuel. In single port hybrids the low regression rate below 1 mm/s causes large L/D exceeding a hundred and small fuel loading ratio falling below 0.3. Multi-port hybrids are a typical solution to solve this problem. However, this solution is not the mainstream in Japan. Another approach is to use high regression rate fuels. For example, a fuel regression rate of 4 mm/s decreases L/D to around 10 and increases the loading ratio to around 0.75. Liquefying fuels such as paraffins are strong candidates for high regression fuels and subject of active research in Japan too. Nakagawa et al. in Tokai University employed EVA (Ethylene Vinyl Acetate) to modify viscosity of paraffin based fuels and investigated the effect of viscosity on regression rates. Wada et al. in Akita University employed LTP (Low melting ThermoPlastic) as another candidate of liquefying fuels and demonstrated high regression rates comparable to paraffin fuels. Hori et al. in JAXA/ISAS employed glycidylazide-poly(ethylene glycol) (GAP-PEG) copolymers as high regression rate fuels and modified the combustion characteristics by changing the PEG mixing ratio. Regression rate improvement by changing internal ballistics is another stream of research. The author proposed a new fuel configuration named "CAMUI" in 1998. CAMUI comes from an abbreviation of "cascaded multistage impinging-jet" meaning the distinctive flow field. A CAMUI type fuel grain consists of several cylindrical fuel blocks with two ports in axial direction. The port alignment shifts 90 degrees with each other to make jets out of ports impinge on the upstream end face of the downstream fuel block, resulting in intense heat transfer to the fuel. Yuasa et al. in Tokyo Metropolitan University employed swirling injection method and improved regression rates more than three times higher. However, regression rate distribution along the axis is not uniform due to the decay of the swirl strength. Aso et al. in Kyushu University employed multi-swirl injection to solve this problem. Combinations of swirling injection and paraffin based fuel have been tried and some results show very high regression rates exceeding ten times of conventional one. High fuel regression rates by new fuel, new internal ballistics, or combination of them require faster fuel-oxidizer mixing to maintain combustion efficiency. Nakagawa et al. succeeded to improve combustion efficiency of a paraffin-based fuel from 77% to 96% by a baffle plate. Another effective approach some researchers are trying is to use an aft-chamber to increase residence time. Better understanding of the new flow fields is necessary to reveal basic mechanisms of regression enhancement. Yuasa et al. visualized the combustion field in a swirling injection type motor. Nakagawa et al. observed boundary layer combustion of wax-based fuels. To understand detailed flow structures in swirling flow type hybrids, Sawada et al. (Tohoku Univ.), Teramoto et al. (Univ. of Tokyo), Shimada et al. (ISAS), and Tsuboi et al. (Kyushu Inst. Tech.) are trying to simulate the flow field numerically. Main challenges are turbulent reaction, stiffness due to low Mach number flow, fuel regression model, and other non-steady phenomena. Oshima et al. in Hokkaido University simulated CAMUI type flow fields and discussed correspondence relation between regression distribution of a burning surface and the vortex structure over the surface.

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