• Title/Summary/Keyword: Methoxy poly(ethylene glycol)

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Preparation of Gemcitabine-Loaded Methoxy Poly(ethylene glycol)-b-Poly(L-lactide) Microparticles Using W/O/W Double Emulsion (W/O/W 다중유화법을 이용한 젬시타빈 함유 Methoxy Poly(ethylene glycol)-b-Poly(L-lactide) 미립자 제조)

  • Ryu, Jong-Hoon;Jung, In-Il;Lee, Ji-Eun;Lim, Gio-Bin
    • KSBB Journal
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    • v.26 no.4
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    • pp.333-340
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    • 2011
  • In this study, gemcitabine-loaded methoxy poly(ethylene glycol)-b-poly(L-lactide) (MPEG-PLLA) microparticles with different PEG block lengths were prepared by a W/O/W double emulsion technique. The present study focuses on the investigation of the influence of various preparative parameters such as the ratio of internal water phase and oil phase, polymer concentration, solvent composition of organic phase and salt concentration of external water phase on the morphology and encapsulation efficiency of the microparticles. The microparticles fabricated at high volume ratios of internal water phase to oil phase and at high polymer concentrations showed a relatively high encapsulation efficiency and low porosity. When a dichloromethane/ethyl acetate mixture was used as solvent, both the encapsulation efficiency and drug loading of the microparticles decreased as the level of ethyl acetate increased. The addition of a salt (NaCl) to the external water phase significantly improved the encapsulation efficiency up to 40%, and the microparticles became more spherical with their size and porosity decreased.

Synthesis and Characterization of Thermosensitive Poly(organophosphazenes) with Methoxy-Poly(ethylene glycol) and Alkylamines as Side Groups

  • Lee, Bae-Hoon;Lee, Young-Moo;Sohn, Yoon-Soo;Song, Soo-Chang
    • Bulletin of the Korean Chemical Society
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    • v.23 no.4
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    • pp.549-554
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    • 2002
  • Thermosensitive poly(organophosphazenes) bearing methoxy-poly(ethylene glycol) (MPEG) and alkylamines as substituents have been synthesized and characterized by elemental analysis, NMR spectroscopy, GPC, and DSC. All the polymers exhibited crystallinity, which was probably induced by the MPEG side chain of the polymers. All the polymers exhibited the lower critical solution temperature (LCSTs) in the range of 28 to $94^{\circ}C$ depending on several factors such as mole ratio of the substituents, kinds of PEG and alkylamines. The higher content of MPEG and shorter chain length of alkylamines of the polymers afforded the higher LCST. The LCSTs of the polymers exhibited almost concentration-independent behavior in the range of 3-30 wt % of the polymers in aqueous solutions. The polymers showed the higher LCSTs in the acidic solutions than in the neutral and basic solutions. The ionic strength of the polymer solution affected the LCST, which decreased with increased NaCl concentration. The polymer bearing almost equimolar substitutuents with the -N-P-N- unit has shown the LCST more sensitive to NaCl and pH than that with the -N-P-O- unit. The polymers were found to degrade in acidic solution but be very stable in alkali solution as well as in the buffer solution of pH 7.4.

Characterizations and Release Behavior of Poly [(R)-3-hydroxy butyrate]-co-Methoxy Poly(ethylene glycol) with Various Block Ratios

  • Jeong, Kwan-Ho;Kwon, Seung-Ho;Kim, Young-Jin
    • Macromolecular Research
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    • v.16 no.5
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    • pp.418-423
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    • 2008
  • Poly[(R)-3-hydroxy butyrate] (PHB) and methoxy poly(ethylene glycol) (mPEG) were conjugated by the transesterification reaction with tin(II)-ethylhexanoate (Sn(Oct)-II) as a catalyst. Hydrophobic PHB and hydrophilic mPEG formed an amphiphilic block copolymer which was formed with the self-assembled polymeric micelle in aqueous solution. In this study, we tried to determine the optimum ratio of hydrophobic/hydrophilic segments for controlled drug delivery. The particle size and shape of the polymeric micelle were measured by atomic force microscopy (AFM) and transmission electron microscopy (TEM). Their size were 61-102 nm with various block ratios. Griseofulvin was loaded in the polymeric micelle as a hydrophobic model drug. The loading efficiency and release profile were measured by high performance liquid chromatography (HPLC). The model drug in our system was constantly released for 48 h.

Thermosensitive Sol-gel Phase Transition Behavior of Methoxy poly(ethylene glycol)-b-poly($\varepsilon$-caprolactone) Diblock Copolymers (메톡시 폴리(에틸렌 글리콜)-폴리($\varepsilon$-카프로락톤) 공중합체의 온도감응성 솔-젤 전이 거동)

  • 서광수;박종수;김문석;조선행;이해방;강길선
    • Polymer(Korea)
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    • v.28 no.4
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    • pp.344-351
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    • 2004
  • Poly(ethylene glycol)-based diblock and triblock polyester copolymers stimulating to temperature were studied as injectable biomaterials in drug delivery system because of their nontoxicity, biocompatibility and biodegradability. We synthesized the diblock copolymers consisting of methoxy poly(ethylene glycol) (MPEG) (M$_{n}$=750 g/mole) and poly($\varepsilon$-caprolactone) (PCL) by ring opening polymerization of $\varepsilon$-CL with MPEG as an initiator in the presence of HCl . Et$_2$O. The aqueous solution of synthesized diblock copolymers represented sol phase at room temperature and a sol to gel phase transition as the temperature increased from room temperature to body temperature. To confirm the in vivo gel formation, we observed the formation of gel in the mice body after injection of 20 wt% aqueous solution of each block copolymer. After 2 months, we observed the maintenance of gel without dispersion in mice. In this study, we synthesized diblock copolymers exhibiting sol-gel phase transition and confirmed the feasibility as biomaterials of injectable implantation.n.

Preparation of UV protective cotton fabrics by novel UV-curing technique - Using a photocrosslinkable polymer, poly(ethylene glycol) dimethacylate -

  • Kim, Sin-Hee
    • Journal of Fashion Business
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    • v.11 no.6
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    • pp.52-61
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    • 2007
  • To increase the ultraviolet radiation (UVR) protection of cotton fabric, ultraviolet protection (UVP) materials were treated onto cotton fabric using a new technique, UV-curing. A photocrosslinkablepolymer, poly(ethylene glycol) dimethacrylate was used as a UV-curable resin in the presence of a small amount of photoinitiator. Two kinds of UVP materials were used, UV-absorber, 2,2'-dihydroxy-4-methoxy benzophenone, and UV-scatterer, $TiO_2/ZnO$ Pad-dry-cure method in employing these materials onto cotton was also conducted to compare the effectiveness and the washfastness of UVP treatment between curing methods. UVP treated cotton fabric showed a moderate increase in UVP in case of 2,2'-dihydroxy-4-methoxy benzophenone treatment and a high increase in case of $TiO_2/ZnO$. UV-curing method increased the washfastness of UVP property of $TiO_2/ZnO$ treated cotton fabrics. However, in case of 2,2'-dihydroxy-4-methoxy benzophenone, similar wash fastnesses of UV-cured and pad-dry-cured cotton were observed. It can be presumed that 2,2'-dihydroxy-4-methoxy benzophenone was not significantly affected by water since its hydrophobicity. In short, UV-curing of UVP materials onto cotton was successfully done, and treated cotton fabrics showed the increased UVP properties and an increased washfastness in some extent.

pH-Induced Micellization of Biodegradable Block Copolymers Containing Sulfamethazine

  • Shim, Woo-Sun;Lee, Jae-Sung;Lee, Doo-Sung
    • Macromolecular Research
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    • v.13 no.4
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    • pp.344-351
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    • 2005
  • pH-sensitive block copolymers were synthesized by coupling reaction of sulfamethazine and amphiphilic diblock copolymer, and their micellization-demicellization behavior was investigated. Sulfamethazine (SM), a derivative of sulfonamide, was introduced as a pH responsive moiety while methoxy poly(ethylene glycol)poly(D,L-lactide) (MPEG-PDLLA) and methoxy poly(ethylene glycol)-poly($D,L-lactide-co-{\varepsilon}-caprolactone$) (MPEG-PCLA) were used as biodegradable amphiphilic diblock copolymers. After the sulfamethazine was carboxylated by the reaction with succinic anhydride, the diblock copolymer was conjugated with sulfamethazine by coupling reaction in the presence of DCC. The critical micelle concentration (CMC) and mean diameter of the micelles were examined at various pH conditions through fluorescence spectroscopy, dynamic light scattering and transmission electron microscopy. For MPEG-PDLLA-SM and MPEG-PCLA-SM solutions, the pH-dependent micellization-demicellization was achieved within a narrow pH band, which was not observed in the MPEG-PDLLA and MPEG-PCLA solutions. The micelle showed a spherical morphology and had a very narrow size distribution. This pH-sensitive block copolymer shows potential as a site-targeted drug carrier.

Removal of Pollutants using Amphiphilic Polymer Nanoparticles in Micellar-Enhanced Utrafiltration (한외여과공정에서 양쪽성 고분자 나노파티클을 이용한 오염물 제거)

  • Shim Jin-Kie;Noh Sang-Il;Lee Sang-Bong;Cho Kye-Min;Lee Young-Moo
    • Membrane Journal
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    • v.16 no.1
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    • pp.59-67
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    • 2006
  • Biodegradable amphiphilic polymer was synthesized for removing hydrophobic pollutants(phenol, 4-nitrophenol, benzene, and toluene) and metal ions ($Cs^{+},\;Mg^{2+},\;Cu^{2+},\;Ni^{2+}$, and $Cr^{3}$). The methoxy poly(ethylene glycol)s with different molecular weights (1,100 and 5,000) were used as a hydrophilic segment. The rejection ratio improved in the relatively high molecular weight of MPEG. The rejection ratio of biodegradable nanoparticles without pollutants was over 98%. In removal of hydrophobic pollutants, the rejection ratio increased with the hydrophobic properties. The electron valence affects the rejection ratio of metal ions, indicating rejection ratio was ordered as $3^{+}>2^{+}>1^{+}$.

A Polymeric Micellar Carrier for the Solubilization of Biphenyl Dimethyl Dicarboxylate

  • Chi, Sang-Cheol;Yeom, Dae-Il;Kim, Sung-Chul;Park, Eun-Seok
    • Archives of Pharmacal Research
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    • v.26 no.2
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    • pp.173-181
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    • 2003
  • A polymeric micelle drug delivery system was developed to enhance the solubility of poorly-water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The block copolymers consisting of poly(D,L-lactide) (PLA) as the hydrophobic segment and methoxy poly(ethylene glycol) (mPEG) as the hydrophilic segment were synthesized and characterized by NMR, DSC and MALDI-TOF mass spectroscopy. The size of the polymeric micelles measured by dynamic light scattering showed a narrow monodisperse size distribution with the average diameter less than 50 nm. The MW of mPEG-PLA, 3000 (MW of mPEG, 2 K; MW of PLA, 1K), and the presence of hydrophilic and hydrophobic segments on the polymeric micelles were confirmed by MALDI-TOF mass spectroscopy and NMR, respectively. Polymeric micelle solutions of DDB were prepared by three different methods, i.e. the matrix method, emulsion method and dialysis method. In the matrix method, DDB solubility was reached to 13.29 mg/mL. The mPEG-PLA 2K-1K micelle system was compared with the poloxamer 407 micelle system for their critical micelle concentration, micelle size, solubilizing capacity, stability in dilution and physical state. DDB loaded-polymeric micelles prepared by the matrix method showed a significantly increased aqueous solubility (>5000 fold over intrinsic solubility) and were found to be superior to the poloxamer 407 micelles as a drug carrier.

Effect of Poly(ethylene glycol)Grafting on Polyethylenimine as a Gene Transfer Vector in vitro

  • Choe, Jin Hui;Choe, Jun Sik;Seo, Hye Ran;Park, Jong Sang
    • Bulletin of the Korean Chemical Society
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    • v.22 no.1
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    • pp.46-52
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    • 2001
  • To evaluate the non-ionic polymer, poly(ethylene glycol) (PEG), as a component in cationic copolymers for non-viral gene delivery systems, PEG was coupled to polyethylenimine (PEI). We present the effects of different degrees and shapes of pegylation of PEI on cytotoxicity, water solubility and transfection efficiency. This work reports the synthesis and characterization of a series of cationic copolymers on the basis of the conjugates of PEI with PEG. The modified molecules were significantly less toxic than the original polymer. Moreover, the chemical modification led to enhancement of their solubility. The comparison of pegylated PEIs with different degrees of derivation showed that all the polymers tested reached comparable levels of transgene expression to that of native PEI. As assessed by agarose gel electrophoresis, even highly substituted PEI derivatives were still able to form polyionic complexes with DNA. However, aside from an increase in solubility and retention of the ability to condense DNA, methoxy-PEG-modified PEIs resulted in a significant decrease in the transfection activity of the DNA complexes. In fact, the efficiency of the copolymer was compromised even at a low degree of modification suggesting that the PEG action resulting from its shape is important for efficient gene transfer. The mode of PEG grafting and the degree of modification influenced the transfection efficiency of PEI.

Methotrexate-Incorporated Polymeric Micelles Composed of Methoxy Poly(ethylene glycol)-Grafted Chitosan

  • Jeong, Young-Il;Seo, Dong-Hyuk;Kim, Don-Gon;Choi, Chang-Yong;Jang, Mi-Kyeong;Nah, Jae-Woon;Park, Yoon-Kyung
    • Macromolecular Research
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    • v.17 no.7
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    • pp.538-543
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    • 2009
  • In this study, methotrexate (MTX)-encapsulated polymeric micelles using methoxy poly(ethylene glycol) (MPEG)-grafted chitosan (ChitoPEG) copolymer were prepared. The MIX-incorporated polymeric micelles of ChitoPEG copolymer has a particle size of around 50-100 nm. In 1H nuclear magnetic resonance (NMR) study, the specific peaks of MTX disappeared in heavy water ($D_2O$) and only the specific peak of MPEG was observed, while all of the peaks were confirmed in dimethyl sulfoxide (DMSO). These results indicated that MTX was complexed with chitosan and then formed an ion complex inner-core of the polymeric micelle in an aqueous environment. The drug contents of the polymeric micelle were around $4{\sim}12%$ and the loading efficiency of MTX in the polymeric micelles was higher than 60% (w/w) for all of the formulations. The cytotoxicity of MIX and MTX-incorporated polymeric micelle against CT26 tumor cells was not significantly changed.