• Macromolecular Research
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• v.14 no.4
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• pp.461-465
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• 2006

Two types of injectable system using thermosensitive chitosan (chitosan-g-NIPAAm), hydrogel and microparticles (MPs)-embedded hydrogel were developed as drug carriers for controlled release and their pharmaceutical potentials were investigated. 5-Fluorouracil (5-FU)-loaded, biodegradable PLGA MPs were prepared by a double emulsion method and then simply mixed with an aqueous solution of thermosensitive chitosan at room temperature. All 5-FU release rates from the hydrogel matrix were faster than bovine serum albumin (BSA), possibly due to the difference in the molecular weight of the drugs. The 5-FU release profile from MPs-embedded hydrogel was shown to reduce the burst effect and exhibit nearly zero-order release behavior from the beginning of each initial stage. Thus, these MPs-embedded hydrogels, as well as thermosensitive chitosan hydrogel, have promising potential as an injectable drug carrier for pharmaceutical applications.

• Journal of Powder Materials
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• v.30 no.1
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• pp.47-52
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• 2023

The purpose of this study is to develop and evaluate amorphous spray-dried microparticles (SDM) containing levosulpiride to increase its solubility. SDM are prepared via solvent evaporation using polyvinylpyrrolidone (PVP) as the water-soluble polymer and Cremophor RH40 as the surfactant. The SDM is prepared by varying the amounts of PVP and Cremophor RH40, and its physicochemical properties, solubility, and dissolution are confirmed. All levosulpiride-loaded SDMs converted the crystalline drug into an amorphous form, significantly improving drug solubility and dissolution compared with the drug alone. SDM consisting of drug/PVP/Cremophor RH40 in a weight ratio of 5:10:3, with increased solubility (720 ± 36 vs. 1822 ± 51 ㎍/mL) and dissolution rate (10.3 ± 2.2 vs. 92.6 ± 6.0%) compared with drug alone, shows potential as a commercial drug for improved oral bioavailability of levosulpiride.

• Korean Chemical Engineering Research
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• v.46 no.2
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• pp.222-226
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• 2008

Nanoparticles have been developed and applied for various applications to intelligently deliver bioactive materials. Herein, lactocin was processed into nanoparticles with methacrylic acid-methyl methacrylate copolymer (1:1) (eudragit L100). The eudragit polymer can protect lactocin from the stomach acid and release lactocin in the intestines. When acetone and pH 7 buffer solution were used as non-solvent and solvent, respectively, the smallest volume-average particle size (290 nm) could be obtained. Freeze drying in presence of carrageenan (dispersant) can process the particles into dried powders with minimum aggregation. SEM observation revealed the primary particles prepared based on lactocin and eudragit were of a few tens of nanometers.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.293-299
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• 2000

Biodegradable microspheres made from poly-lactide-co-glycolide polymers have been considered as a new delivery system for single-dose vaccine. Purified tetanus toxoid (TT) was encapsulated in poly-lactide(PLA) and poly-lactide-co-glycolide (PLGA) microparticles using a solvent evaporation method in a multiple emulsion system (water-in oil-in water). The morphology of 77-loaded microparticles was spherical and the suface of them was smooth. The particle size was in a range of 2-10. Protein loading efficiency was 68-97.8%. PLGA (85:15) microparticle showed the highest efficiency. Protein release pattern was influenced by polymer molecular weight and composition. The release rate of PLA(Mw 100,000) microsphere was higher than any other microspheres. In consequence of the hydrolysis of PLGA(50:50) microspheres, environmental pH decreased from 7.4 to 5.0. The PLA, PLGA (75:25) and PLGA (85:15) microshperes showed no significant pH change. The antigenicity or n in microshperes was assayed by indirect sandwich ELISA using equine polyclonal tetanus antitoxin for capture antibody and human polyclonal tetanus antitoxin for primary antibody. The antigenicity of TT in PLA (Mw 100,000), PLGA(50:50, Mw 100,000) and PLGA (75:25, Mw 73,300) after 30 days incubation showed 54, 40.9 and 76.7%, respectively.

• Polymer(Korea)
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• v.31 no.2
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• pp.168-176
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• 2007

The sub-micron particles of poly ($\gamma-glutamic$ acid) (PGA) containing lysozyme have been prepared using supercritical antisolvent (SAS) precipitation process at various experimental conditions such as pressure, temperature, inner diameter of nozzle, and concentration. As overall results of the application of SAS process to this system, the smaller size powder has been produced as (i) increasing pressure, (ii) decreasing temperature, (iii) decreasing the inner diameter of nozzle, and (iv) decreasing the concentration of PGA and lysozyme. It is found by means of FT-IR analysis that during SAS process, the composition has changed from the original composition of PGA : lysozyme=50 : 50 into PGA : lysozyme=33 : 67 at final product powder. It means that PGA has higher solubility for the mixed solvent of carbon dioxide and dimethyl sulfoxide (DMSO). Due to such difference of solubility, this particle forms the core-shell structure of which the core consists mainly of lysozyme. It is also found that the residual DMSO amount of $7.8\times10^{-3}wt%$ exists inside the powder.

• Clean Technology
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• v.25 no.4
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• pp.283-288
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• 2019

Monodisperse microparticles has been particularly enabling for various applications in the encapsulation and delivery of pharmaceutical agents. The microfluidic devices are attractive candidates to produce highly uniform droplets that serve as templates to form monodisperse microparticles. The microfluidic devices that have micro-scale channel allow precise control of the balance between surface tension and viscous forces in two-phase flows. One of its essential abilities is to generate highly monodisperse droplets. In this paper, a microfluidic approach for preparing monodisperse polycaprolactone (PCL) microparticles is presented. The microfluidic devices that have a flow-focusing generator are manufactured by soft-lithography using polydimethylsiloxane (PDMS). The crucial factors in the droplet generation are the controllability of size and monodispersity of the microdroplets. For this, the volumetric flow rates of the dispersed phase of oil solution and the continuous phase of water to generate monodisperse droplets are optimized. As a result, the optimal flow condition for droplet dripping region that is able to generate uniform droplet is found. Furthermore, the droplets containing PCL polymer by solvent evaporation after collection of droplet from device is solidified to generate the microparticle. The particle size can be controlled by tuning the flow rate and the size of the microchannel. The monodispersity of the PCL particles is measured by a coefficient of variation (CV) below 5%.

• KSBB Journal
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• v.23 no.5
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• pp.452-459
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• 2008

To obtain maximal efficacy with minimal systemic side-effects, many studies have been carried out to achieve the controlled release of 5-fluorouracil (5-FU). In this study, biodegradable poly(L-lactide) (L-PLA) microparticles containing 5-FU were prepared by a process, called aerosol solvent extraction system (ASES), utilizing supercritical carbon dioxide. The effects of various organic solvents, drug/polymer feeding ratio, polymer molecular weight, and blending with the same polymers with different molecular weights on the formation of 5-FU loaded microparticles were investigated under a predetermined operating condition from our previous study. The drug recovery, entrapment efficiency, and in vitro drug release kinetics were determined by HPLC assays. The drug recovery obtained from the ASES process was found to be very high, whereas the drug entrapment efficiency was considerably low in all the experiments due to the poor affinity between L-PLA and 5-FU. These results indicated that the precipitation rate of L-PLA might be quite different from that of 5-FU so that there was little chance to form 5-FU loaded L-PLA microparticles.

• Journal of Pharmaceutical Investigation
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• v.41 no.3
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• pp.147-151
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• 2011

This paper demonstrates the development of a method for preparing micropatterned microdiscs in order to increase contact area with cells and to change the release pattern of drugs. The microdiscs were manufactured with hot embossing, where a polyurethane master structure was pressed onto both solid and porous microparticles made of polylactic-co-glycolic acid at various temperatures to form a micropattern on the microdiscs. Flat microdiscs were formed by hot embossing of porous microparticles; the porosity allowed space for flattening of the microdiscs. Three types of micro-grooves were patterned onto the flat microdiscs using prepared micropatterned molds: (1) 10 ${\mu}M$ deep, 5 ${\mu}M$ wide, and spaced 2 ${\mu}M$ apart; (2) 10 ${\mu}M$ deep, 9 ${\mu}M$ wide, and spaced 5 ${\mu}M$ apart; and (3) 10 ${\mu}M$ deep, 50 ${\mu}M$ wide, and spaced 50 ${\mu}M$ apart. This novel microdisc preparation method using hot embossing to create micropatterns on flattened porous microparticles provides the opportunity for low-cost, rapid manufacture of microdiscs that can be used to control cell adhesion and drug delivery rates.