• Title/Summary/Keyword: critical aggregation concentration

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Poly(vinyl pyrrolidone) Conjugated Lipid System for the Hydrophobic Drug Delivery

  • Lee, Hye-Yun;Yu, Seol-A;Jeong, Kwan-Ho;Kim, Young-Jin
    • Macromolecular Research
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    • v.15 no.6
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    • pp.547-552
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    • 2007
  • Water soluble polymer, poly(vinyl pyrrolidone) was chosen to conjugate with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-N-(succinyl) (N-succinyl DPPE) to make a new drug delivery system. PVP with an amine group (amino-PVP) was polymerized by free radical polymerization. The amine group of amino-PVP was conjugated with the carboxylic group of N-succinyl DPPE. The resultant conjugate could form nanoparticles in the aqueous solution; these nanoparticles were termed a lipid-polymer system. The critical aggregation concentration was measured with pyrene to give a value of $1{\times}10^{-3}g/L$. The particle size of the lipid-polymer system, as measured by DLS, AFM and TEM, was about 70 nm. Lipophilic component in the inner part of the lipid-polymer system could derive the physical interaction with hydrophobic drugs. Griseofulvin was used as a model drug in this study. The loading efficiency and release profile of the drug were measured by HPLC. The loading efficiency was about 54%. The release behavior was sustained for a prolonged time of 12 days. The proposed lipid-polymer system with biodegradable and biocompatible properties has promising potential as a passive-targeting drug delivery carrier because of its small particle size.

A Phenomenological Study on Micellization and Solubilization (Micelle 형성에 관한 현상학적 고찰)

  • Myung Soo Kim
    • Journal of the Korean Chemical Society
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    • v.33 no.5
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    • pp.459-467
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    • 1989
  • When the sufactants are dissolved in water, they associate to form micelles and solubilize oil inside the micelle to form swollen micelles. Although spherical aggregates like micelles and swollen micelles occupy the same regions in the phase diagram of water-oil-surfactant systems, they are treated in different viewpoint for the formation of such aggregates. Hence a unified thermodynamic formalism for the formation of such structure is presented in this study. In all cases, the to ideal solution theory is applied for dilute system and the energy of formation is expressed as the sum of hydrophobic interaction energy and surface energy due to surfactant film. From the model, critical micelle concentration (CMC), average aggregation number, and solubilization ratio are predicted and compared with the known experimental observation.

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Self-Aggregated Nanoparticles of Lipoic Acid Conjugated Hyaluronic Acid (히알루론산에 결합된 리포산 자기조립체의 제조 및 특성)

  • Hong, In-Rim;Kim, Young-Jin
    • Polymer(Korea)
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    • v.32 no.6
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    • pp.561-565
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    • 2008
  • Hyaluronic acid (HA) is a natural glycosaminoglycan and is used widely in the pharmaceutical field. Lipoic acid (LA) helps the regeneration of exogenous and endogenous antioxidants such as Vitamin C and Vitamin E as well as glutathione. It also acts as antioxidant indirectly. Hydrophilic HA as a biodegradable and biocompatible polymer was conjugated with hydrophobic LA as an antioxidant to form the graft copolymer. The carboxyl group of HA was modified by adipic acid dihydrazide (ADH). The synthesis of HA-g-LA graft copolymers was characterized by FT-IR, $^1H$-NMR spectroscopy. The conjugates could form the self-assembled nanoparticles in aqueous solution. The particle size and critical aggregation concentration were verified to use the nanoparticle as a carrier fur the hydrophobic material.

Preparation and Characterization of Self-aggregated Nanoparticles of Chitosan-Lipoic Acid Conjugate (키토산-리포산 자기 조립체의 제조 및 특성)

  • Park, Eun-Ju;Kim, Young-Jin
    • Polymer(Korea)
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    • v.32 no.6
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    • pp.544-548
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    • 2008
  • The objective of this study is to obtain the anti-oxidant nanoparticles based on biocompatible polymers. It was chosen to conjugate with chitosan as the biodegradable polymer and lipoic acid as the hydrophobic anti-oxidant. Lipoic acid helps the regeneration of exogenous and endogenous anti-oxidants vitamin as well as glutathione and hence acts as antioxidant indirectly. Chitosan was prepared from chitin which was deacetylated under alkali solution for the various reaction time. Lipoic acid-chitosan complex was confirmed by $^1H$-NMR. The critical aggregation concentration was measured using pyrene and the values were about $5{\times}10^{-3}$ g/L. The particle shapes and sizes of the chitosan-lipoic acid nano-particles were about 135 nm that measured by DLS and TEM.

Water-Soluble Distyrylbenzene Fluorophore and Fluorescence Behavior in a Polymeric Vesicle

  • Nayak, Rati Ranjan;Woo, Han-Young
    • Journal of the Korean Chemical Society
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    • v.51 no.6
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    • pp.513-519
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    • 2007
  • A vesicle forming polymer, poly(sodium acrylamidoundecanoate) (PSAU) and a water-soluble distyrylbenzene- based fluorophore, TPADSB-C were synthesized and characterized by using UV-vis and photoluminescence (PL) spectroscopy. An inter-chain vesicle formation of PSAU was observed at ~0.01 g/L from N-phenyl naphthylamine fluorescence measurement with changing PSAU concentration in water. Above critical aggregation concentration of PSAU, optical properties of TPADSB-C were investigated to study the microenvironment modulation through dye incorporation in the polymeric vesicle. The emission of TPADSB-C in the presence of PSAU vesicles was blue-shifted and the PL quantum efficiency was increased to 90% due to the microenvironment (e.g. polarity) change in aqueous solution. This study shows that the polymeric vesicle containing molecular fluorophores has a great potential as an efficient, stable and biocompatible labeling tag in biological cell imaging.

Preparation of a Hydrophobized Chitosan Oligosaccharide for Application as an Efficient Gene Carrier

  • Son Sohee;Chae Su Young;Choi Changyong;Kim Myung-Yul;Ngugen Vu Giang;Jang Mi-Kyeong;Nah Jae-Woon;Kweon Jung Keoo
    • Macromolecular Research
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    • v.12 no.6
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    • pp.573-580
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    • 2004
  • To prepare chitosan-based polymeric amphiphiles that can form nanosized core-shell structures (nanopar­ticles) in aqueous milieu, chitosan oligosaccharides (COSs) were modified chemically with hydrophobic cholesterol groups. The physicochemical properties of the hydrophobized COSs (COSCs) were investigated by using dynamic light scattering and fluorescence spectroscopy. The feasibility of applying the COSCs to biomedical applications was investigated by introducing them into a gene delivery system. The COSCs formed nanosized self-aggregates in aqueous environments. Furthermore, the physicochemical properties of the COSC nanoparticles were closely related to the molecular weights of the COSs and the number of hydrophobic groups per COS chain. The critical aggregation concentration values decreased upon increasing the hydrophobicity of the COSCs. The COSCs effi­ciently condensed plasmid DNA into nanosized ion-complexes, in contrast to the effect of the unmodified COSs. An investigation of gene condensation, performed using a gel retardation assay, revealed that $COS6(M_n=6,040 Da)$ containing $5\%$ of cholesteryl chloroformate (COS6C5) formed a stable DNA complex at a COS6C5/DNA weight ratio of 2. In contrast, COS6, the unmodified COS, failed to form a stable COS/DNA complex even at an elevated weight ratio of 8. Furthermore, the COS6C5/DNA complex enhanced the in vitro transfection efficiency on Human embryonic kidney 293 cells by over 100 and 3 times those of COS6 and poly(L-lysine), respectively. Therefore, hydrophobized chitosan oligosaccharide can be considered as an efficient gene carrier for gene delivery systems.

Viscosity and Density Studies on the Second CMC of the Aqueous Solution of Dodecyl Pyridinium Chloride (粘性度 및 密度測定에 依한 Dodecyle Pyridinium Chloride 水溶液의 第二 CMC에 關한 硏究)

  • Young Won Youn;Kun Moo Lee
    • Journal of the Korean Chemical Society
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    • v.19 no.5
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    • pp.289-293
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    • 1975
  • According to the viscosity and density studies of an aqueous solution of dodecyl pyridinium chloride (DPC) it was shown that the 2nd critical micelle concentration (2nd cmc) existed in the solution in addition to the 1st cmc. The volume fraction ${\phi}_m$ of the hydrated micelle was calculated by using the following equation: ${\Pi}_{rm}=1+2.5{\phi}_m+14.1{\phi}_m^2$ It has been found that the increment of ${\phi}_m$ in the ${\phi}_m$ vs. $C_m$ curve decreased at near the 2nd cmc. And the partial specific volume ($\={v}$) of DPC obtained from the density measurement also decreased rapidly at near the 2nd cmc and remains constant value above the 2nd cmc. This may be attributed to a change in the micelle structure at the 2nd cmc caused by a variation in the type of aggregation and by a decrease in the counterion binding by the micelle.

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The effects of succinylacetone on synthesis of protoporphyrin IX and cell growth of Myxococcus xanthus (Myxococcus xanthus의 protoporphyrin IX의 합성과 세포 성장에 대한 succinylacetone의 영향)

  • 이병욱
    • Journal of Life Science
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    • v.13 no.6
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    • pp.814-821
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    • 2003
  • Protoporphyrin IX is an intermediate molecule in the heme biosynthetic pathway. Intra- and extracellular concentrations of protoporphyrin IX in the wild type strain, Myxococcus xanthus DK1622 were measured by reverse phase HPLC. The amount of intracellular protoporphyrin IX continuously increased and reached 6.4 picomoles/mg of protein at the stationary phase. Extracellular protoporphyrin IX began to be detected from the mid-exponential phase. The culture supernatant that was collected in the stationary phase contained approximately 3.0 picomoles of proto-porphyrin IX per mg of protein. Spores formed by nutrient depletion contained about 6.5 picomole protoporphyrin IX/mg of protein. The synthesis of protoporphyrin IX and cell growth were strongly inhibited by addition of succinylacetone to a final concentration of $500\muM$. Succinylacetone, however did not appear to interfere developmental processes. Normal developmental behaviors including aggregation and spore formation was achieved even if succinylacetone was added in a medium. Photolysis among cells grown on a starvation medium supplemented with succinylacetone was also observed. These results indicate that protoporphyrin IX may be important to M. ,xanthus vegetative growth, but not critical to development processes.

The Effect of Nitric Oxide Donor or Nitric Oxide Synthase Inhibitor on Oxidant Injury to Cultured Rat Lung Microvascular Endothelial Cells (산화질소 공여물과 산화질소 합성효소 길항제가 백서 폐미세혈관 내피세포 산화제 손상에 미치는 영향)

  • Chang, Joon;Michael, John R.;Kim, Se-Kyu;Kim, Sung-Kyu;Lee, Won-Young;Kang, Kyung-Ho;Yoo, Se-Hwa;Chae, Yang-Seok
    • Tuberculosis and Respiratory Diseases
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    • v.45 no.6
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    • pp.1265-1276
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    • 1998
  • Background : Nitric oxide(NO) is an endogenously produced free radical that plays an important role in regulating vascular tone, inhibition of platelet aggregation and white blood cell adhesion to endothelial cells, and host defense against infection. The highly reactive nature of NO with oxygen radicals suggests that it may either promote or reduce oxidant-induced cell injury in several biological pathways. Oxidant injury and interactions between pulmonary vascular endothelium and leukocytes are important in the pathogenesis of acute lung injury, including acute respiratory distress syndrome(ARDS). In ARDS, therapeutic administration of NO is a clinical condition providing exogenous NO in oxidant-induced endothelial injury. The role of exogenous NO from NO donor or the suppression of endogenous NO production was evaluated in oxidant-induced endothelial injury. Method : The oxidant injury in cultured rat lung microvascular endothelial cells(RLMVC) was induced by hydrogen peroxide generated from glucose oxidase(GO). Cell injury was evaluated by $^{51}$chromium($^{51}Cr$) release technique. NO donor, such as S-nitroso-N-acetylpenicillamine(SNAP) or sodium nitroprusside(SNP), was added to the endothelial cells as a source of exogenous NO. Endogenous production of NO was suppressed with N-monomethyl-L-arginine(L-NMMA) which is an NO synthase inhibitor. L-NMMA was also used in increased endogenous NO production induced by combined stimulation with interferon-$\gamma$(INF-$\gamma$), tumor necrosis factor-$\alpha$(TNF-$\alpha$), and lipopolysaccharide(LPS). NO generation from NO donor or from the endothelial cells was evaluated by measuring nitrite concentration. Result : $^{51}Cr$ release was $8.7{\pm}0.5%$ in GO 5 mU/ml, $14.4{\pm}2.9%$ in GO 10 mU/ml, $32.3{\pm}2.9%$ in GO 15 mU/ml, $55.5{\pm}0.3%$ in GO 20 mU/ml and $67.8{\pm}0.9%$ in GO 30 mU/ml ; it was significantly increased in GO 15 mU/ml or higher concentrations when compared with $9.6{\pm}0.7%$ in control(p < 0.05; n=6). L-NMMA(0.5 mM) did not affect the $^{51}Cr$ release by GO. Nitrite concentration was increased to $3.9{\pm}0.3\;{\mu}M$ in culture media of RLMVC treated with INF-$\gamma$ (500 U/ml), TNF-$\alpha$(150 U/ml) and LPS($1\;{\mu}g/ml$) for 24 hours ; it was significantly suppressed by the addition of L-NMMA. The presence of L-NMMA did not affect $^{51}Cr$ release induced by GO in RLMVC pretreated with INF-$\gamma$, TNF-$\alpha$ and LPS. The increase of $^{51}Cr$ release with GO(20 mU/ml) was prevented completely by adding 100 ${\mu}M$ SNAP. But the add of SNP, potassium ferrocyanate or potassium ferricyanate did not protect the oxidant injury. Nitrite accumulation was $23{\pm}1.0\;{\mu}M$ from 100 ${\mu}M$ SNAP at 4 hours in phenol red free Hanks' balanced salt solution. But nitrite was not detectable from SNP upto 1 mM The presence of SNAP did not affect the time dependent generation of hydrogen peroxide by GO in phenol red free Hanks' balanced salt solution. Conclusion : Hydrogen peroxide generated by GO causes oxidant injury in RLMVC. Exogenous NO from NO donor prevents oxidant injury, and the protective effect may be related to the ability to release NO. These results suggest that the exogenous NO may be protective on oxidant injury to the endothelium.

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