• Journal of Pharmaceutical Investigation
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• v.39 no.5
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• pp.333-337
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• 2009

We aimed to optimize the formulation of porcine placental extract (PPE)-loaded liposomes for intramuscular administration and to investigate the effect of surface charges on the muscular retention in mice. PPE-loaded liposomes were formulated to have neutral, anionic, or cationic surface charges. The in vitro release profiles were studied by spectrofluorometry. In vivo distribution patterns at mice were studied using molecular imaging technology. Among the three types of liposomes, 1,2-dioleoyl-3-trimethylammonium-propane and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-based cationic liposomes showed the most prolonged in vitro release profile. Consistent with the in vitro results, the in vivo distribution study revealed that the cationic liposomes were retained at the site of administration for the longest period. Our results suggest the potential of cationic PPE-loaded liposomes for sustained release of the components after intramuscular administration.

• Archives of Pharmacal Research
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• v.12 no.2
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• pp.88-93
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• 1989

In order to obtain some informations about the effect of molecular weight on the release rate of drug from drug carrier, two types of poly-L-glutamic acid (PLGA)-cytarabine (ara-C) conjugates, PLGA-ara-C:I and PLGA-ara-C:II, were synthesized using two types of PLGA having different average molecular weight, 43,000 and 77,800, respectively. The PLGA-ara-C conjugates were synthesized by mixed anhydride method and found to be covalently linked. Both types of conjugates charged negatively at biological pH. The pH-dependent release rate of ara-C was observed in both cases, and the release rate was accelerated in basic, acidic conditions (the k values were 0.015 $day^{-1}$ at pH 7.0, 0.024 $day^{-1}$ at pH 5.0, and 0.059 $day^{-1}$ at pH 9.0 in the case of PLGA-ara-C:I) and in the presence of pretense. The time required for the release of 16.5% of ara-C from PLGA-ara-C:I were 8 hr and 144 hr in the presence and absence of protease, respectively. Although both types of conjugates showed similar drug substitution ratio, they showed different release rates. Between the two types of conjugates, PLGA-ara-C:II showed the faster release rate (0.030 vs 0.042 $day^{-1}$ in pH 7.4 phosphate buffer solution at $37^{\circ}C$) and the smaller activation energy for the release of drug (12.5 vs 7.7 Kcal/mol) than PLGA-ara-C:I. The characteristic effect of molecular weight on the release rates of PLGA-ara-C conjugates suggests that the drug release rate might be effectively controlled over a prolonged period of time by the combined use of the different types of PLGA-ara-C conjugates having different molecular weights.

• Korean Journal of Environmental Agriculture
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• v.42 no.2
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• pp.112-120
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• 2023

Methane (CH₄) and nitrous oxide (N₂O) are significant contributors to greenhouse gas (GHG) emissions from rice fields. Mid-summer drainage is a commonly practiced water management technique that reduces CH₄ emissions from rice fields. Slow-release fertilizers gradually release nutrients over an extended period and have been shown to reduce N₂O emissions. However, the combined effect of slow-release fertilizer and water management on GHG emissions remains unclear. This study compared GHG emissions from a rice paddy subjected to mid-summer drainage for 10 days (control) with that of a rice paddy subjected to prolonged mid-summer drainage for 20 days combined with slow-release fertilizer (W+S). Gas sampling was conducted weekly using a closed chamber method. During the rice cultivation period, cumulative CH₄ and N₂O emissions were reduced by 12.3% and 16.2%, respectively, in the W+S treatment compared to the control. Moreover, the W+S treatment exhibited a 1.9% increase in grain yield compared to the control. Under experimental conditions, slow-release fertilizers, in combination with prolonged mid-summer drainage, proved to be the optimal approach for achieving high crop yield while reducing GHG emissions. This represents an effective strategy to mitigate GHG emissions from rice paddy fields.

• Asian-Australasian Journal of Animal Sciences
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• v.9 no.1
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• pp.57-61
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• 1996

Four castrated Corriedale sheep were used in an experiment to observe the changes in insulin, growth hormone and cortisol in blood plasma following a prolonged infusion of a high rate of somatostatin (SRIF). The animals wee infused with either saline, 25 or $50{\mu}g/kg/h$ of SRIF for 3 hours. Blood samples wee taken every 20 minutes until 1 hour following the end of the SRIF infusion. Both SRIF infusion levels suppressed the release of insulin into plasma to approximately 3.5 mU/l. The SRIF infusions reduced the concentration of growth hormone to barely detectable levels. Following the withdrawal of SRIF there was a massive release of growth hormone. The plasma concentration of growth hormone reached 60 ng/ml within 20 minutes, the length of the growth hormone discharge was in excess of 1 hour. The extent of the discharge of growth hormone following the SRIF infusions was greater than that suppressed by the infusion. The SRIF apparently caused an increase in the plasma concentration of cortisol at the end of the infusion and following is withdrawal. This is possibly associated with some change in the metabolic rate associated with the suppression of insulin or glucagons release. The present experiment demonstrates that a high rate of SRIF infusion can not completely inhibit the release of insulin into the plasma.

• Journal of Pharmaceutical Investigation
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• v.41 no.5
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• pp.279-288
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• 2011

The Dexamethasone (DEX) loaded chitosan microspheres were prepared by thermal denaturation and chemical cross-linking method using a dierent concentration of glutaraldehyde as chemical cross-linking agent. The prepared microspheres were evaluated for the percentage of Drug Loading (DL), Encapsulation Efficiency (EE) and surface morphology by Scanning Electron Microscopy (SEM). DL and EE were found to be maximum range of 10.0 to 10.79 % and 58.19 to 64.73 % respectively. The SEM Photographs of the resultant microspheres exhibited fairly smooth surfaces and predominantly spherical in appearance. In addition, Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) shown that there was no interaction between the drug and polymer. In vitro and in vivo release studies revealed that the release of dexamethasone was sustained and extended up to 63 days and effectively controlled by the extent of cross-linking agent. Non-clinical parameters such as paw volume, hematological parameters like Erythrocyte Sedimentation Rate (ESR), Paced Cell Volume (PCV), Total Leucocytes Count (TLC), Hemoglobin (Hb), Differential Cell Count (DCC) were investigated in Fruend's Complete Adjuvant (FCA) induced arthritic rats. Radiology and histopathological studies were also performed in order to evaluate the therapeutic efficacy of the DEX-loaded microspheres in extenuating the rat arthritic model.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.19 no.2
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• pp.108-117
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• 2006

The oxidative notification of low density lipoprotein(LDL) has been implicated in the development of atherosclerosis. Oxidized LDL are found in macrophage foam cell, and it can induce an macrophage proliferation in atherosclerotic plaque. In this study, we investigated the hypothesis that Samkieum may reduce atherosclerosis by lowering the oxidiazability of LDL, To achieve this goal, we examined the effect of Samkieum on LDL oxidation nitric oxide production in mouse macrophage cell line, RAW264.7, and the effect of Samkieum on cupuric sulfate-induced cytotoxicity, LDH release, and macrophage activity. Samkieum inhibited the generation of oxidized LDL from native LDL in RAW264.7 cell culture, and decreased the release of LDH from cupric sulfate-stimulated RAW264.7 cell. In other experiments, Samkieum activated RAW264.7 cell, and prolonged the survival time, and increased nitric oxide production in Raw 264.7 cells.

• YAKHAK HOEJI
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• v.39 no.1
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• pp.48-54
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• 1995

Coupling of tetracycline(Tc) to dithiocarbamate chitosan(DTCC) via chelate bond was investigated varying reaction time, concentration, temperature, pH, and Ca(II)/Tc ratio. The amount of Tc bound to matrix increased to give a maximum and decreased as the reaction proceeded. The degree and rate of dissociation of Tc complex were affected by the reaction temperature, and pH. By running the reaction at low temperature and pH, the degree of dissociation was greatly diminished. Properties of drug-release from DTCC-Ca(II)-Tc complex were studied by batch- and flow-method and release of Tc and CA(II) by flow method followed nearly zero-order. DTCC-Ca(II)-Tc showed very prolonged antimicrobial activity compared to that of free Tc.

• Journal of Society of Preventive Korean Medicine
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• v.5 no.1
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• pp.134-143
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• 2001

The oxidative modification of low density lipoprotein(LDL) has been implicated in the development of atherosclerosis. Oxidized LDL are found in macrophage foam cell, and it can induce an macrophage proliferation in atherosclerotic plaque. In this study, we investigated the hypothesis that gamisoyosan(GS) may reduce atherosclerosis by lowering the oxidiazability of LDL, To achive this goal, we examined the effect of GS on LDL oxidation, nitric oxide production in mouse macrophage cell line, RAW264.7, and the effect of GS on cupuric sulfate-induced cytotoxicity, LDH release, and macrophage activity. GS inhibited the generation of oxidized LDL from native LDL in RAW264.7 cell culture, and decreased the release of LDH from cupric sulfate-stimulated RAW264.7 cell. In other experiments, GS activated RAW264.7 cell, and prolonged the survival time, and increased nitric oxide production in Raw 264.7 cells.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.279.1-279.1
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• 2002

Accumulation of ceramide mass in MCF-7 cells by the anti-cancer agent. paclitaxel. was found to occur primarily due to activation of the de novo synthesis pathway. Morever. the addition of paclitaxel resulted in the accumulation of ceramide, which was followed by a prolonged arachidonic acid release. Participation of ceramide de novo pathway in arachidonate signaling was detected since L-cycloserine, an inhibitor of de novo synthesis, was able to inhibit the paclitaxel-induced AA release and cytotoxicity. (omitted)

• Polymer(Korea)
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• v.26 no.1
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• pp.128-138
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• 2002

1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU, Carmustine)-loaded poly(D, L-lactide-co-glycolide) (PLGA, lactide/glycolide mole ratio 75 : 25) microparticles were prepared and fabricated into wafers in an attempt to study the possibility for the treatment of malignant glioma by direct inserting the wafers to the tumor or the cavity remained after surgical resection of the tumor. SEM observation of the microparticles prepared by spray drying method revealed that the microparticles were spherical, i. e. microspheres. Significant reduction of the crystallinity of BCNU encapsulated in PLGA was confirmed by X-ray diffraction and differential scanning calorimetry analyses of the BCNU-loaded PLGA microparticles. Release pattern of BCNU was dependent on several preparation parameters, such as the molecular weight and concentration of PLGA, and initial BCNU loading amount, etc. In vitro release of BCNU was prolonged over 8 weeks with close to zero-order release pattern after initial burst effect. Observations of morphological change of wafers and pH change of release media during release test period confirmed that hydration and degradation of PLGA would be facilitated with an increase of BCNU-loading amount.