• Journal of Pharmaceutical Investigation
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• v.31 no.4
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• pp.257-263
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• 2001

The microspheres have been developed as a new drug delivery system. Although many particulate drug carriers, such as liposome, niosome and emulsion, have been introduced, injectable and biodegradable microspheres appears to be a particularly ideal delivery system because the local anesthesia is not necessary for the insertion of large implants and for the removal of the device after the drug release is finished. Biodegradable microspheres with nicotine and triamcinolone acetonide are prepared and evaluated. As biodegradible polymers, PLA (M.W. 15,000, PLA-0015), PLGA (M.W. 17,000, RG 502) and PLGA (M.W. 8,600, RG 502H) are used. This study attempted to prepare and evaluate the nicotine and triamcinolone acetonide-incorporated microspheres, which were prepared by two methods, solvent-evaporation and spray-drying methods. The microspheres, as a disperse system for injections, were evaluated by particle size, size distribution, entrapment efficiency, and in vitro drug release patterns. The differences of preparation method, partition coefficient, types of polymer, and preparation conditions of microspheres influence the particle size, entrapment efficiency, and in vitro drug release patterns.

• Macromolecular Research
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• v.16 no.8
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• pp.717-724
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• 2008

In this study, we prepared all-trans retinoic acid (ATRA)-encapsulated, surfactant-free, PLGA nanoparticles. The nanoparticles were formed by nanoprecipitation process, after which the solvent was removed by solvent evaporation or dialysis method. When a nanoparticle was prepared by the nanoprecipitation - solvent evaporation method, the nanoparticles were bigger than the nanoparticles of the nanoprecipitation - dialysis method, despite the higher although loading efficiency. Nanoparticles from the nanoprecipitation - dialysis method were smaller than 200 nm in diameter, while the loading efficiency was not significantly changed. Especially, nanoparticles prepared from DMAc, 1,4-dioxane, and DMF had a diameter of less than 100 nm. In the transmission electron microscopy (TEM) observations, all of the nanoparticles showed spherical shapes. The loading efficiency of ATRA was higher than 90% (w/w) at all formulations with exception of THF. The drug content was increased with increasing drug-feeding amount while the loading efficiency was decreased. In the drug release study, an initial burst was observed for $2{\sim}6$ days according to the variations of the formulation, after which the drug was continuously released over one month. Nanoparticles from the nanoprecipitation - dialysis method showed faster drug release than those from the nanoprecipitation - solvent evaporation method. The decreased drug release kinetics was observed at lower drug contents. In the tumor cell cytotoxicity test, ATRA-encapsulated, surfactant-free, PLGA nanoparticles exhibited similar cytotoxicity with that of ATRA itself.

• 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.

• Journal of the Korean Ceramic Society
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• v.33 no.1
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• pp.17-24
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• 1996

Pb(Mg1/3Nb2/3)O3 powder with high purity chemical homogeniety and reactivity was prepared by solvent eva-poration of common solution. The common solution was fabricated using a Pb(NO3)2 Mg(NO)3 and NB solution which was prepared by dissolving NbC in H2O2 acquous solution. In precusor powder prepared by solvent evaporation method the synthetic temperature of Pb(Mg1/3 Nb2/3)O3 phase was lowered. And the formation of homogeneous Pb(Mg1/3Nb2/3)O3 phase was enhanced but the formation of pyrochlore phase was reduced. The dielectric constant of PMN ceramics from the synthesized powder was found to increase with both sintering temperature and excess MgO and subsequent analysis of the microstructures confirmed that this was due to an increase in grain size. The grain size dependence is explained as a consequence of low-permittivity grain boundaries.

• Bulletin of the Korean Chemical Society
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• v.33 no.10
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• pp.3208-3212
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• 2012

Controlled drug delivery systems employing microparticles offer lots of advantages over conventional drug dosage formulations. Microencapsulation technique have been conducted with biodegradable polymers such as poly(lactic-co-glycolic acid) (PLGA) and poly(lactic acid) (PLA) for its adjustable biodegradability and biocompatibility. In this study, we evaluated two techniques, oil-in-water (o/w) emulsion solvent evaporation and spray drying, for preparation of polymeric microparticles encapsulating a newly synthesized drug, SS-AG20, for the long-term drug delivery of this low-molecular-weight drug with a very short half-life. Drug-loaded microparticles prepared by the solvent evaporation method showed a smoother morphology; however, relatively poor encapsulation efficiency and drastic initial burst were discovered as drawbacks. Spray-dried drug-loaded microparticles had an imperfect surface with pores and distorted portions so that its initial burst was critical (70.05-87.16%) when the preparation was carried out with a 5% polymeric solution. By increasing the concentration of the polymer, the morphology was refined and undesirable initial burst was circumvented (burst was reduced to 35.93-74.85%) while retaining high encapsulation efficiency. Moreover, by encapsulating the drug with various biodegradable polymers using the spray drying method, gradual and sustained drug release, for up to 2 weeks, was achieved.

• Macromolecular Research
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• v.11 no.3
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• pp.183-188
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• 2003

The controlled delivery of anticancer agents using biodegradable polymeric implant has been developed to solve the problem of penetration of blood brain barrier and severe systemic toxicity. This study was performed to prepare 5-FU-loaded poly (L-lactide-co-glycolide) (PLGA) wafer fabricated microparticles prepared by two different method and to evaluate their release profile for the application of the treatment of brain tumor. 5-FU-loaded PLGA microparticles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). SEM observation of the 5-FU-loaded PLGA microparticles prepared by rotary solvent evaporation method showed that 5-FU was almost surrounded by PLGA and significant reduction of crystallinity of 5-FU was confirmed by XRD. In case of release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by mechanical mixing, the release profile of 5-FU followed near first order release kinetics. In contrast to the above result, release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by rotary solvent evaporation method followed near zero order release kinetics. These results indicate that preparation method of the 5-FU-loaded PLGA microparticles to fabricate into wafers was contributed to drug release profile.

• Archives of Pharmacal Research
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• v.13 no.4
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• pp.293-297
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• 1990

Sustained release microspheres containing phenylpropanolamine HCI (PPA) were prepared with acrylic polymer (Eudragit RL/RS) sand hydroxypropylmethylcellulose phthalate (HPMCP) using a emulsion-solvent evaporation method. Magnesium strate was used a smoothing agent for preparation of microspheres. The microspheres obtained were very spherical and free-flowing particles. Scanning electron microscopy showed that microspheres have a smooth surface and a sponage-like internal structure. The dissolution rate of PPA from the microspheres was dependent on the pH of dissolution media. PPA showed faster relase in hP 1. 2 solution than in pH 7.4 solution due to the solubility of PPA. Therefore we prepared new microspheres containing 5% (w/v) HPMCP in order to control the release of PPA. The release rate of PPA from these new microspheres was similar in pH 1.2 and pH 7.4 solution.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.612-618
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• 2005

A mucoadhesive microsphere was prepared by an interpolymer complexation and solvent evaporation method, using chitosan and poly(acrylic acid) (PAA), to prolong the gastric resid ence time of the delivery system. The Fourier transform infrared results showed that microspheres were formed by an electrostatic interaction between the carboxyl groups of the PAA and the amine groups of the chitosan. X-ray diffraction and differential scanning calorimetry analysis showed that the enrofloxacin in the chitosan-PAA microsphere was molecularly dispersed in an amorphous state. Scanning electron microscopy of the surface and the quantity of mucin attached to the microspheres indicated that chitosan-PAA microspheres had a higher affinity for mucin than those of chitosan alone. The swelling and dissolution of the chitosan-PAA microspheres were found to be dependent on the pH of the medium. The rate of enrofloxacin released from the chitosan-PAA microspheres was slower at higher pH; therefore, based on their mucoadhesive properties and morphology, the chitosan-PAA microspheres can be used as a mucoadhesive oral drug delivery system.

• Journal of Pharmaceutical Investigation
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• v.24 no.2
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• pp.85-94
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• 1994

Inclusion complexes of ketoconazole (KT) with ${\alpha}-$, ${\beta}-cyclodextrin$ (CD) and dimethyl-${\beta}-cyclodextrin$ $(DM{\beta}CD)$ in a molar ratio of 1:2 were prepared by freeze-drying and solvent evaporation methods. The interactions of KT with ${\alpha}-CD$, ${\beta}-CD$ and $DM{\beta}CD$ in aqueous solution and in solid state were investigated by solubility study, infrared (lR) spectroscopy and differential scanning calorimetry (DSC). The stability constant of $KT-DM{\beta}CD$ inclusion complex (lC) was found to be the largest among three inclusion complexes. Clear differences in IR spectra and DSC curves were observed between inclusion complexes and physical mixtures (PM) of KT-CDs. It was also shown by IR spectra and DSC curves that solvent evaporation method might be. superior to the freeze-drying method in preparing the inclusion complexes of KT-CDs. The dissolution rate of KT was markedly increased by inclusion complex formation with CDs in the buffer solution at pH 4.0 and pH 6.8. The mean dissolution time (MDT,min), which represents the rapidity of dissolution, was in the order of $KT-DM{\beta}CD$ IC (3.20) < $KT-{\beta}-CD$ IC (4.36) < $KT-{\alpha}-CD$ IC (6.99) < $KT-{\alpha}-CD$ PM (17.46)< $KT-{\beta}-CD$ PM (19.36) < $KT-{\beta}-CD$ PM (28.53). The dissolution rates of KT-CD ICsprepared by solvent evaporation method were faster than those of KT-CD ICs prepared by freeze-drying method.

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.315.1-315.1
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• 2001