• Journal of Pharmaceutical Investigation
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• v.26 no.4
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• pp.273-280
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• 1996

Chondroitin sulfate/gelatin microspheres containing dexamethasone 21-acetate were prepared by complex coacervation method and their release patterns were examined in vitro. Microspheres prepared with a small amount of crosslinking agent had smooth surface and few pores, but those with a large amount of crosslinking agent were more porous and less spherical. In vitro release patterns were varied by changing polymer/drug weight ratio and amount of crosslinking agent. The release rate of dexamethasone 21-acetate in the presence of collagenase was faster than that in the absence of collagenase. Anti-inflammatory effect of dexamethasone 21-acetate microspheres was more efficient than that of dexamethasone 21-acetate solution in carrageenan-induced arthritis in the rat. On the basis of the above results, we might expect the degradation and drug release rate of these microspheres to be regulated by the degree of crosslinking and the level of enzymes. In patients with severe rheumatoid arthritis who have high concentration of collagenase, more drug would be released from the microspheres. An intra-articular injection therapy of rheumatoid arthritis with desired release kinetics could be developed to enhance patient compliance and therapeutic index.

• Journal of Microbiology and Biotechnology
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• v.27 no.9
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• pp.1617-1627
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• 2017

Dietary approaches using structured lipids, including medium-chain fatty acids and diacylglycerols, have been adopted for the prevention of obesity-induced chronic inflammation. In an extension to previous studies, medium-chain fatty acid-diacylglycerol enriched dietary oil (MCDG) was prepared by interesterification of canola oil and medium-chain fatty acid-triacylglycerols. The consequent MCDG product was applied to RAW264.7 macrophages followed by the assessment of multiple inflammatory responses. Compared with conventionally used canola and olive oil controls, MCDG suppressed macrophage phagocytosis, as assessed by the uptake of microsphere beads. Furthermore, the production of IL-6 and $TNF-{\alpha}$, transcription of COX-2 and iNOS, and expression of CD80 on cell surfaces were downregulated by MCDG in LPS-stimulated macrophages. Subsequently, differentiated 3T3-L1 adipocytes were evaluated for proinflammatory cytokine production and lipid accumulation. IL-6 production was marginally affected and lipid accumulation was inhibited by MCDG. Taken together, these results suggest that MCDG has potential as an alternative oil for cooking in order to prevent obesity-induced inflammation.

• Macromolecular Research
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• v.8 no.2
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• pp.80-88
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• 2000

Biodegradable microspheres were prepared with poly(L-lactide-co-glycolide) (PLGA, 75 : 25 by mole ratio) by an oil/oil solvent evaporation method for the sustained release of anti-AIDS virus agent, AZT The microspheres of relatively narrow size distribution (7.6$\pm$ 3.8 ㎛) were obtained by controlling the fabrication conditions. The shape of microspheres prepared was smooth and spherical. The efficiency of AZT loading into the PLGA microsphere was over 93% compared to that below 15% for microspheres by a conventional water/oil/water method. The effects of Preparation conditions on the morphology and in vitro AZT release pattern were investigated. in vitro release studies showed that different release pattern and release rates could be achieved by simply modifying factors in the fabrication conditions such as the type and amount of surfactant, initial amount of loaded drug, the temperature of solvent evaporation, and so on. PLCA microspheres prepared by 5% of initial drug loading, 1.0% (w/w) of surfactant concentration, and 25$\^{C}$ of solvent evaporation temperature were free from initial burst effect and a near-zero order sustained release was observed. Possible mechanisms of the near-zero order sustained release for our system have been proposed.

• YAKHAK HOEJI
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• v.39 no.5
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• pp.487-494
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• 1995

Solid lipid microspheres (SLMs) were prepared using various lipids and solidifying agents, in order to enhance the gastrointestinal absorption of Cyclosporine A (Cs A) which is a practically water-insoluble drug with low systemic bioavailability. Egg lecithin and HCO-60 (polyoxyethylated 60 mol, hydrogenated castor oil) were used as lipids. Stearic acid and stearyl alcohol were used as solidifying agents. Emulsion concentrates containing Cs A were prepared by mixing the melted lipid and solidifying agent with water, employing bile salts as a cosurfactant. SLMs were obtained by dispersing the warm emulsion concentrate in cold distilled water under mechanical stirring, followed by freeze drying. Physical characteristics of each SLM were investigated by particle size analysis, optical microscopy and scanning electron microscopy. Mean particle size of SLMs was in the range of 30 to 40.mu.m. The SLMs were in good appearance with spherical shape before freeze drying, but were deformed partially after freeze drying. Drug loading efficiencies of SLMs were observed as high as 80 to 90% in average. The systemic bioavailability of Cs A from different SLM formula was investigated in rats following oral administration. Cs A in whole blood was extracted and assayed by HPLC. SLMs revealed the higher bioavailabilities than the standard formula based on the marketed product. SLMs might have several advantages over standard formula for enhanced gastrointestinal absorption, controlled release properties, high loading capacity of the water-insoluble drug, and feasibility of solid dosage forms with better stability in storage.

• Elastomers and Composites
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• v.58 no.4
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• pp.208-215
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• 2023

In this study, the properties of polyurethane-polydimethylsiloxane (PU-PDMS) hybrid foams containing different types and contents of physical blowing agents (PBAs) were investigated. Two types of blowing agents, namely physical blowing agents and thermally expandable microspheres (TEM), were applied. The apparent density was measured using precisely cut foam samples, and the pore size was measured using image software. In addition, the microstructure of the foam was confirmed via scanning electron microscopy and transmission electron microscopy. The thermal conductivities related to the microstructures of the different foams were compared. When 0.5 phr of the hydrocarbon-based PBA was added, the apparent density and pore size of the foam were minimal; however, the pore size was larger than that of neat foam. In contrast, the addition of 3 phr of TEM effectively reduced both the apparent density and pore size of the PBAs. The increase in resin viscosity owing to TEM could enhance bubble production stability, leading to the formation of more uniform and smaller pores. These results indicate that TEM is a highly efficient PBA that can be employed to decrease the weight and pore size of PU-PDMS hybrid foams.

• Membrane Journal
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• v.14 no.3
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• pp.218-229
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• 2004

We prepared monodispersed calcium alginate microspheres by controlling various conditions of emulsification procedure using a lab-scale batch type membrane emulsification system equipped with SPG (Shirasu porous glass) tubular membranes. We determined the effects of process parameters of membrane emulsification (ratio of dispersed phase to continuous phase, alginate concentration, emulsifier concentration, type and concentration of stabilizer, transmembrane pressure, concentration of crosslinking agent, stirring speed and membrane pore size) on the mean size and size distribution of alginate microspheres. The increase of the ratio of dispersed phase to continuous phase, transmembrane pressure and alginate concentration led to the increase in the mean size of alginate microspheres. On the contrary, the increase in emulsifier concentration, stirring speed of the continuous phase and concentration of the crosslinking agent caused the reduction of the mean size of microspheres. Through controlling these parameters, monodisperse alginate microspheres with about $6{\mu}{\textrm{m}}$ of the mean size and 1.1 of the size distribution value were finally prepared in case of the using SPC membrane with the pore size of $2.9{\mu}{\textrm{m}}$.

• Proceedings of the Korean Vacuum Society Conference
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• 2016.02a
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• pp.360.1-360.1
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• 2016

Hydroxyapatite (Ca10(PO4)6(OH)2, HAP) particles have attracted a great deal of attention in biomedical fields due to their good biocompatibility, bioactivity and fairly broad applications as drug delivery, dental implant, bone cement, and etc. Thus, many researchers have made an effort to add new functionalities such as luminescence, drug delivery, and bone regeneration properties up to HAP powders by controlling their nanostructure as well as composition. In this research, the mesoporous strontium substituted HAP (Sr-HAP) microspheres were synthesized using a hydrothermal method. In this synthesis, aspartic acid monomers were utilized to form microsphere by controlling surface energy of HAP particles and Sr ions were substituted into Ca ion sites, which induced luminescence property in HAP powders. Moreover, the change in the amount of Sr substitution was found to influence the particle size, morphology, and concurrently surface area, which led to changing drug loading as well as drug release property. The amount of Sr influences the morphology, luminescent properties, particle size, surface area cell viability and drug loading property, which are investigated by SEM, TEM, XRD, FTIR, BET, XPS and in vitro test such as MTT assay and drug release test. In particular, the multifunctional Sr-HAP with molar ratios of 0.25 (Sr/(Ca+Sr)) possessed the strongest luminescent property as well as the superior drug loading and sustained release properties that were correspondent with large surface area and pore size. Our study indicates that the fabricated multifunctional Sr-HAP microspheres are quite useful for bone regeneration and drug delivery.

• Korean Chemical Engineering Research
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• v.56 no.4
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• pp.461-468
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• 2018

Microspheres were prepared by solvent-evaporation method with Poly-L-lactic acid (PLLA) as a starting material, and the effects of preparation variables on microsphere shape and average particle size were investigated. As the concentration of PVA solution increased from 1 to 5 wt%, the average particle size decreased from $370{\mu}m$ to $160{\mu}m$ and then increased to $240{\mu}m$ at 7 wt%. On the other hand, As the addition volume of PVA solution increased from 10 mL to 50 mL, the average particle size decreased from $370{\mu}m$ to $220{\mu}m$. Also, as the stirring speed increased from 500 rpm to 1,500 rpm, the average particle size decreased from $370{\mu}m$ to $110{\mu}m$. When dichloromethane and chloroform were used as organic solvents, respectively, the average particle size did not show any significant difference. However, when dichloromethane was used, voids were observed on the particle surface, but when chloroform was used, smooth spherical particles were obtained.

• KSBB Journal
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• v.16 no.5
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• pp.505-510
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• 2001

The preparation, characterization and drug release behaviour of drug(indomethacin) loaded Poly(L-lactic acid)(PLA), tarmarind acetate and levan acetate mircospheres were investigated. Hydrophobic tarmarind acetate and levan acetate were prepared by chemical modification of hydrophilic tarmaried gum and levan and microspheres were made by a solvent evaporation method. In the case of poly(L-lactic acid) microspheres, drug release rate was effected by polymer-drug ratios and drum release was sustained by increasing of polymer content. The yield of microspheres were effected by many factors and the mean size was below 1 $\mu$m, The IND release profiles from tarmarind acetate and levan acetate micropheres were more slightly less than ploy(L-lactic acid) microspheres.

• Journal of Pharmaceutical Investigation
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• v.19 no.4
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• pp.195-202
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• 1989

In attempt to improve the chemotherapeutic activity of adriamycin, adriamycin-entrapped HSA microspheres were prepared and investigated by the various in vitro experiments. The shape, surface characteristics and size distribution of HSA microspheres are observed by scanning electron microscopy. The in vitro drug release, albumin matrix degradation by protease of HSA microspheres were studied. The shape of HSA microspheres were spherical and the surface was smooth and compact. The size of HSA microspheres ranged from 0.4 to $2.5\;{\mu}m$ and have average diameters of 0.5 to $0.7\;{\mu}m$. The size distribution of HSA microspheres prepared by ultrasonication was mainly affected by albumin concentration and heating time in the process of hardening. In in vitro, almost all adriamycin was released from HSA microspheres for 8 hr. Analysis of the resulting adriamycin release profiles demonstrated that adriamycin is released from the microspheres in two distinct steps, a fast phase (until 30 min) followed by a much slower sustained release phase. Drug release, which is due to diffusion, was depended on the rate of matrix hydration. Drug release was largely affected by albumin concentration and heating temperature during the process of hardening. Albumin matrix degradation of HSA microspheres was affected by heating temperature and albumin concentration. Higher temperature and longer times generally produce harder, less porous, and slowly degradable microspheres.