• Title/Summary/Keyword: sustained loading

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Preparation of Biodegradable PLGA Microspheres for Sustained Local Anesthesia and Their in vitro Release Behavior (지속적인 국소마취를 위한 생분해성 PLGA 미립구의 제조와 생체외 방출 거동)

  • 조진철;강길선;최학수;이종문;이해방
    • Polymer(Korea)
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    • v.24 no.5
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    • pp.728-735
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    • 2000
  • Fentanyl-loaded biodegradable poly(L-lactide-co-glycolide) (75 : 25 by mole ratio of lactide to glycolide, PLGA) microspheres (MSs) were prepared to study the possibility for long-acting local anesthesia. We developed the fentanyl base (FB, slightly water-soluble)-loaded PLGA MSs by means of conventional O/W solvent evaporation method. The size of MSs was in the range of 10~150 ${\mu}{\textrm}{m}$. The morphology of MSs was characterized by SEM, and the in vitro release amounts of FB were analyzed by HPLC. The lowest porous cross-sectional morphology and the highest encapsulation efficiency were obtained by using gelatin as an emulsifier. The influences of several preparation parameters, such as emulsifier types, molecular weights and concentrations of PLGA, and initial drug loading amount, etc., have been observed in the release patterns of FB. The release of FB in vitro was more prolonged over 25 days, with close to zero-order pattern by controlling the preparation parameters. We also investigated the physicochemical properties of FB-loaded PLGA MSs by X-ray diffraction and differential scanning calorimeter.

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Controlled Release of Nerve Growth Factor from Sandwiched Poly(L-lactide-co-glycolide) Films for the Application in Neural Tissue Engineering

  • Gilson Khang;Jeon, Eun-Kyung;John M. Rhee;Lee, Ilwoo;Lee, Sang-Jin;Lee, Hai-Bang
    • Macromolecular Research
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    • v.11 no.5
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    • pp.334-340
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    • 2003
  • In order to fabricate new sustained delivery device of nerve growth factor (NGF), we developed NGF-loaded biodegradable poly(L-lactide-co-glycolide) (PLGA, the mole ratio of lactide to glycolide 75:25, molecular weight: 83,000 and 43,000 g/mole, respectively) film by novel and simple sandwich solvent casting method for the possibility of the application of neural tissue engineering. PLGA was copolymerized by direct condensation reaction and the molecular weight was controlled by reaction time. Released behavior of NGF from NGF-loaded films was characterized by enzyme linked immunosorbent assay (ELISA) and degradation characteristics were observed by scanning electron microscopy (SEM) and gel permeation chromatography (GPC). The bioactivity of released NGF was identified using a rat pheochromocytoma (PC-12) cell based bioassay. The release of NGF from the NGF-loaded PLGA films was prolonged over 35 days with zero-order rate of 0.5-0.8 ng NGF/day without initial burst and could be controlled by the variations of molecular weight and NGF loading amount. After 7 days NGF released in phosphate buffered saline and PC-12 cell cultured on the NGF-loaded PLGA film for 3 days. The released NGF stimulated neurite sprouting in cultured PC-12 cells, that is to say, the remained NGF in the NGF/PLGA film at 37 $^{\circ}C$ for 7 days was still bioactive. This study suggested that NGF-loaded PLGA sandwich film is released the desired period in delivery system and useful neuronal growth culture as nerve contact guidance tube for the application of neural tissue engineering.

Preparation and Characterization of Pamidronate-loaded PLGA Wafer for the Treatment of Bone Resorption (골 재흡수 치료를 위한 파미드로네이트를 함유한 이식형 생분해성 PLGA 웨이퍼의 제조와 특성결정)

  • 유제영;김상욱;강길선;성하수;정제교
    • Polymer(Korea)
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    • v.26 no.5
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    • pp.680-690
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    • 2002
  • Implantable biodegradable wafers were prepared with pamidronate -loaded poly (L-lactide-co-glycolide) (PLGA, 75 : 25 mole ratio by lactide to glycolide, molecular weight : 20000 and 90000 g/mole) by direct compression method for the sustained release of pamidronate to investigate the possibility for the treatment of bone resorption. Pamidronate-loaded PLGA powders were prepared by means of physical mixing and spray drying with the control of formulation factors and characterized by scanning electron microscope and X-ray diffractometer. The pamidronate-loaded PLGA powders fabricated into wafers by direct compression under the constant pressure and time at room temperature. These wafers were also observed for their structural characteristic, release pattern, and degradation pattern. The release rate of pamidronate increased with increasing their initial loading ratio as well as increasing wafer thickness. The molecular weight of PLGA affects the release pattern : the higher molecular weight of PLGA, the faster release rate. It can be explained that the higher viscosity of high molecular PLGA solution at same concentration tends to aggregate PLGA and pamidronate resulting in unstable pharmaceutical dosage form. This system had advantages in terms of simplicity in design and obviousness of drug release rate and nay be useful as an implantable dosage form for the treatment of aural cholesteatoma.

Structural behavior of the stiffened double-skin profiled composite walls under compression

  • Qin, Ying;Li, Yong-Wei;Lan, Xu-Zhao;Su, Yu-Sen;Wang, Xiang-Yu;Wu, Yuan-De
    • Steel and Composite Structures
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    • v.31 no.1
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    • pp.1-12
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    • 2019
  • Steel-concrete composite walls have been proposed and developed for applications in various types of structures. The double-skin profiled composite walls, as a natural development of composite flooring, provide structural and architectural merits. However, adequate intermediate fasteners between profiled steel plates and concrete core are required to fully mobilize the composite action and to improve the structural behavior of the wall. In this research, two new types of fasteners (i.e., threaded rods and vertical plates) were proposed and three specimens with different fastener types or fastener arrangements were tested under axial compression. The experimental results were evaluated in terms of failure modes, axial load versus axial displacement response, strength index, ductility index, and load-strain relationship. It was found that specimen with symmetrically arranged thread rods sustained more stable axial strain than that with staggered arranged threaded rods. Meanwhile, vertical plates are more suitable for practical use since they provide stronger confinement to profiled steel plate and effectively prevent the steel plate from early local buckling, which eventually enhance the composite action and increase the axial compressive capacity of the wall. The calculation methods were then proposed and good agreement was observed between the test results and the predicted results.

Docetaxel-loaded PLGA nanoparticles to increase pharmacological sensitivity in MDA-MB-231 and MCF-7 breast cancer cells

  • Tran, Phuong;Nguyen, Thu Nhan;Lee, Yeseul;Tran, Phan Nhan;Park, Jeong-Sook
    • The Korean Journal of Physiology and Pharmacology
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    • v.25 no.5
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    • pp.479-488
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    • 2021
  • This study aimed to develop docetaxel (DTX) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and -26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The in vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC50 values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

Antibacterial activity of florfenicol composite nanogels against Staphylococcus aureus small colony variants

  • Liu, Jinhuan;Ju, Mujie;Wu, Yifei;Leng, Nannan;Algharib, Samah Attia;Luo, Wanhe
    • Journal of Veterinary Science
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    • v.23 no.5
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    • pp.78.1-78.13
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    • 2022
  • Background: Florfenicol might be ineffective for treating Staphylococcus aureus small colony variants (SCVs) mastitis. Objectives: In this study, florfenicol-loaded chitosan (CS)-sodium tripolyphosphate (TPP) composite nanogels were prepared to allow targeted delivery to SCV infected sites. Methods: The formulation screening, the characteristics, in vitro release, antibacterial activity, therapeutic efficacy, and biosafety of the florfenicol composite nanogels were studied. Results: The optimized formulation was obtained when the CS and TPP were 10 and 5 mg/mL, respectively. The encapsulation efficiency, loading capacity, size, polydispersity index, and zeta potential of the optimized florfenicol composite nanogels were 87.3% ± 2.7%, 5.8% ± 1.4%, 280.3 ± 1.5 nm, 0.15 ± 0.03, and 36.3 ± 1.4 mv, respectively. Optical and scanning electron microscopy showed that spherical particles with a relatively uniform distribution and drugs might be incorporated in cross-linked polymeric networks. The in vitro release study showed that the florfenicol composite nanogels exhibited a biphasic pattern with the sustained release of 72.2% ± 1.8% at 48 h in pH 5.5 phosphate-buffered saline. The minimal inhibitory concentrations of commercial florfenicol solution and florfenicol composite nanogels against SCVs were 1 and 0.25 ㎍/mL, respectively. The time-killing curves and live-dead bacterial staining showed that the florfenicol composite nanogels were concentration-dependent. Furthermore, the florfenicol composite nanogels displayed good therapeutic efficacy against SCVs mastitis. Biological safety studies showed that the florfenicol composite nanogels might be a biocompatible preparation because of their non-toxic effects on the renal tissue and liver. Conclusions: Florfenicol composite nanogels might improve the treatment of SCV infections.

Cell clusters in intervertebral disc degeneration: an attempted repair mechanism aborted via apoptosis

  • Polly Lama;Jerina Tiwari;Pulkit Mutreja;Sukirti Chauhan;Ian J Harding;Trish Dolan;Michael A Adams;Christine Le Maitre
    • Anatomy and Cell Biology
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    • v.56 no.3
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    • pp.382-393
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    • 2023
  • Cell clusters are a histological hallmark feature of intervertebral disc degeneration. Clusters arise from cell proliferation, are associated with replicative senescence, and remain metabolically, but their precise role in various stages of disc degeneration remain obscure. The aim of this study was therefore to investigate small, medium, and large size cell-clusters. For this purpose, human disc samples were collected from 55 subjects, aged 37-72 years, 21 patients had disc herniation, 10 had degenerated non-herniated discs, and 9 had degenerative scoliosis with spinal curvature <45°. 15 non-degenerated control discs were from cadavers. Clusters and matrix changes were investigated with histology, immunohistochemistry, and Sodium dodecyl sulphate polyacrylamide gel electrophoresis (SDS-PAGE). Data obtained were analyzed with spearman rank correlation and ANOVA. Results revealed, small and medium-sized clusters were positive for cell proliferation markers Ki-67 and proliferating cell nuclear antigen (PCNA) in control and slightly degenerated human discs, while large cell clusters were typically more abundant in severely degenerated and herniated discs. Large clusters associated with matrix fissures, proteoglycan loss, matrix metalloproteinase-1 (MMP-1), and Caspase-3. Spatial association findings were reconfirmed with SDS-PAGE that showed presence to these target markers based on its molecular weight. Controls, slightly degenerated discs showed smaller clusters, less proteoglycan loss, MMP-1, and Caspase-3. In conclusion, cell clusters in the early stages of degeneration could be indicative of repair, however sustained loading increases large cell clusters especially around microscopic fissures that accelerates inflammatory catabolism and alters cellular metabolism, thus attempted repair process initiated by cell clusters fails and is aborted at least in part via apoptosis.

Characteristic Community Dynamics of Phyto- and Zooplankton in a Shallow Eutrophoic Reservoir (얕은 부영양 저수지의 동${\cdot}$식물플랑크톤 군집변화 특성)

  • Kim, Ho-Sub;Kong, Dong-Soo;Hwang, Soon-Jin
    • Korean Journal of Ecology and Environment
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    • v.38 no.1 s.110
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    • pp.18-29
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    • 2005
  • This study was conducted to understand seasonal dynamics of phyto- and zooplankton communities in a shallow eutrophic reservoir (Shingu reservoir) from November 2002 to February 2004. Cyanophyceae dominated throughout the year, except for spring (March ${\sim}$ May) when Bacillariophyceae (Melosira varians) and Chlorophyceae (Dictyosphaerium puchellum) were dominant. The change of dominant species in Cyanophytes occurred in June and December 2003, and the increase of phytoplankton cell density in July and November was observed when the P loading through two inflows was high. In May, Oscillatoria spp. and Aphanizomenon sp. were dominant, but replaced by Microcystis spp. in the end of May. Dominant Microcystis spp. sustained until December and shifted to Oscillatoria spp. and Aphanizomenon sp. TN/TP ratio ranged from 13 to 46 (Avg. $27{\pm}6$) from June to December when cyanobacteria (Microcystis spp.) dominated. Rotifers such as Keratella cochlearis, Keratella valga, Polyarthra spp., Conochilus unicornis, Pompholyx complanata dominated in average 67.8% of the zooplankton community. Abundance of zooplankton was the highest in June 2003, when Pompholyx complanata (12,388 ind $L^{-1}$) was dominant. In May, the significant increase of Conochilus unicornis biomass ($1,048{\pm}28\;{\mu}g\;C\;L^{-1}$) was observed with distinct improvement of transparency ($Z_{eu}/\;Z_m=\;1.1$). These results suggest that the seasonal variation of phytoplankton communities in this reservoir are to be understood as results of multi-interactive factors such as temperature, light condition and nutrients, and small-sized rotifers as important predator.

Life Assessment of Gas Turbine Blade Based on Actual Operation Condition (실 운전조건을 고려한 가스터빈 블레이드 수명평가)

  • Choi, Woo Sung;Song, Gee Wook;Chang, Sung Yong;Kim, Beom Soo
    • Transactions of the Korean Society of Mechanical Engineers A
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    • v.38 no.10
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    • pp.1185-1191
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    • 2014
  • Gas turbine blades that have complex geometry of the cooling holes and cooling passages are usually subjected to cyclic and sustained thermal loads due to changes in the operating characteristic in combined power plants; these results in non-uniform temperature and stress distributions according to time to gas turbine blades. Those operation conditions cause creep or thermo-mechanical fatigue damage and reduce the lifetime of gas turbine blades. Thus, an accurate analysis of the stresses caused by various loading conditions is required to ensure the integrity and to ensure an accurate life assessment of the components of a gas turbine. It is well known that computational analysis such as cross-linking process including CFD, heat transfer and stress analysis is used as an alternative to demonstration test. In this paper, temperatures and stresses of gas turbine blade were calculated with fluid-structural analysis integrating fluid-thermal-solid analysis methodologies by considering actual operation conditions. Based on analysis results, additionally, the total lifetime was obtained using creep and thermo-mechanical damage model.

Absorption Study of Genistein Using Solid Lipid Microparticles and Nanoparticles: Control of Oral Bioavailability by Particle Sizes

  • Kim, Jeong Tae;Barua, Sonia;Kim, Hyeongmin;Hong, Seong-Chul;Yoo, Seung-Yup;Jeon, Hyojin;Cho, Yeongjin;Gil, Sangwon;Oh, Kyungsoo;Lee, Jaehwi
    • Biomolecules & Therapeutics
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    • v.25 no.4
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    • pp.452-459
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    • 2017
  • In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.