• Biomaterials and Biomechanics in Bioengineering
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• v.2 no.2
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• pp.85-96
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• 2015

This study developed biodegradable bi-layered drug-eluting beads and investigated the in-vitro release of fluorouracil and cisplatin from the beads. To manufacture the drug-eluting beads, poly[(d,l)-lactide-co-glycolide] (PLGA) with lactide:glycolide ratios of 50:50 and 75:25 were mixed with fluorouracil or cisplatin. The mixture was compressed and sintered at $55^{\circ}C$ to form bi-layered beads. An elution method was employed to characterize the release characteristic of the pharmaceuticals over a 30-day period at $37^{\circ}C$. The influence of polymer type (i.e., 50:50 or 75:25 PLGA) and layer layout on the release characteristics was investigated. The experiment suggested that biodegradable beads released high concentrations of fluorouracil and cisplatin for more than 30 days. The 75:25 PLGA released the pharmaceuticals at a slower rate than the 50:50 PLGA. In addition, the bi-layered structure reduced the release rate of drugs from the core layer of the beads. By adopting the compression sintering technique, we will be able to manufacture biodegradable beads for long-term drug delivery of various anti-cancer pharmaceuticals.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.417.1-417.1
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• 2002

The in vitro release of rhGH from PLGA microspheres was characterized. rhGH-loaded PLGA microspheres were prepared with 50:50 poly(D.L-lactide-co-glycolide) (PLGA) polymers using a double emulsion process. To simulate rhGH release under physiological conditions. the microspheres were suspended in a physiological buller at 37$^{\circ}C$. Quantification of the rhGH released and its molecular form analysis were carried out using SE-HPLC. (omitted)

• Polymer(Korea)
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• v.32 no.3
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• pp.246-250
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• 2008

Colloidal stability of the biodegradable nanoparticle was characterized by measuring the variation of particle size with time using photon correlation spectroscopy. Three kinds of polymers, namely, poly(D,L-lactide-co-glycolide)(PLGA), PLGA/poly(L-lactide) blends, and PLGA/poly(L-lactide)-g-poly(ethylene glycol) blends were used as matrix material for nanoparticle preparation. Nanoparticles were prepared with or without using poly(vinyl alcohol)(PVA) as suspension stabilizer to evaluate the condition of preparation. Nanoparticles from the blend of amphiphilic graft copolymer with short poly(ethylene glycol) chain and PLGA maintained suspension for 1 day when protein stock solution was introduced. This is somewhat improvement in colloidal stability against protein adsorption compared with that of nanoparticles without PEG moiety. Suspension stabilizer, PVA, had a significant effect on the colloidal stability against freezing and protein adsorption which led to coagulation of nanoparticles. It is important to consider effect of suspension stabilizer as well as materials used to prepare nanoparticle on the colloidal stability.

• Polymer(Korea)
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• v.36 no.3
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• pp.326-331
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• 2012

In this study, expanded poly(tetrafluoro ethylene) (ePTFE) graft was modified to be used as a hemodialysis vascular access. Biodegradable poly(D,L-lactide-$co$-glycolide) (PLGA) was coated onto the inner surface of ePTFE graft with paclitaxel, which is often used as an anti-cancer agent and for reducing neointimal hyperplasia. Surface characterization before and after PLGA coating was carried out by SEM and ATR-FTIR. Porous sturcture of ePTFE was maintained after coating of PLGA solution. The amounts of coated PLGA and paclitaxel determined by ATR-FTIR and HPLC were 1.96 and 0.263 mg/$cm^2$, respectively. Young's modulus was decreased and tensile strength was increased by PLGA coating. Released paclitaxel as a function of incubation time was monitored by HPLC. Approximately 35% of coated paclitaxel was released steadily for 4 weeks with the biodegradation of PLGA. From these results, it is expected that the effect of paclitaxel on reducing neointimal hyperplasia and stenosis is maintained for a long time.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.417.2-418
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• 2002

The rhGH-loaded PLGA microsphere formulation was prepared using a double emulsion process from hydrophilic 0:50 poly(D.L-lactide-co-glycolide) (PLGA) polymers. To investigate the sustained efficacy of this formulation, ts pharmacodynamic characteristics were analyzed. It showed particle size of ca 53.1 $\mu\textrm{m}$ with high drug ncorporation efficiency and it was sucutaneously administrated to hypophysectomized rats and whole body rowth responses of this formulation were compared to those of the different dosing patterns of rhGH. (omitted)

• The Journal of Korean Academy of Prosthodontics
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• v.46 no.6
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• pp.620-627
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• 2008

STATEMENT OF PROBLEM: A biochemical approach for surface modification has offered an alternative for physicochemical and morphological methods to obtain desirable bone-implant interfaces. PURPOSE: The purpose of the present study was to investigate cell responses to poly (D,L-lactide-co-glycolide) (PLGA)/$1{\alpha}$,25-(OH)$_2D_3$ coating with reference to cellular proliferation and differentiation in vitro. MATERIAL AND METHODS: 96 titanium discs were fabricated and divided into four groups. Group 1 was anodized under 300 V as control. Group 2, 3 and 4 were anodized then coated with 3 ml PLGA/$1{\alpha}$,25-(OH)$_2D_3$ solutions. Amount of the solutions were 2 ul, 20 ul and 200ul respectively. The osteoblast-like Human Osteogenic Sarcoma (HOS) cells were seeded and cultured for 1, 3 and 7 days. MTSbased cell proliferation assay and ALPase activity test were carried out. RESULTS: PLGA nanoparticles were observed as fine, smooth and round and HOS cells attached to the anodized surfaces through strand-like and sheet-like filopodia. After 3 days of culture, the dendritic filopodia were exaggerated and sheet-like cytoplasmic projections covered the coated titanium surfaces. After 3 days of culture, all of the groups showed increased cellular proliferation and the lowest proliferation rate was measured on group 2. Higher amount of incorporated $1{\alpha}$,25-(OH)$_2D_3$ (Group 3 and 4) improved cellular proliferation but the differences were not significant statistically (P > .05). But they increased the rate of ALP activities than the control group at day 3 (P < .05). CONCLUSION: Biodegradable PLGA nanoparticles incorporated with vitamin D metabolite positively affected proliferation and differentiation of cells on the anodized titanium surface.

• Journal of Pharmacopuncture
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• v.19 no.1
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• pp.37-44
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• 2016

Objectives: This study examined the relative efficacies of a derivative of betulinic acid (dBA) and its poly (lactide-co-glycolide) (PLGA) nano-encapsulated form in A549 lung cancer cells in vivo and in co-mutagen [sodium arsenite (SA) + benzo[a]pyrene (BaP)]-induced lung cancer in mice in vivo. Methods: dBA was loaded with PLGA nanoparticles by using the standard solvent displacement method. The sizes and morphologies of nano-dBA (NdBA) were determined by using transmission electron microscopy (TEM), and their intracellular localization was verified by using confocal microscopy. The binding and interaction of NdBA with calf thymus deoxyribonucleic acid (CT-DNA) as a target were analyzed by using conventional circular dichroism (CD) and melting temperature (Tm) profile data. Apoptotic signalling cascades in vitro and in vivo were studied by using an enzyme-linked immunosorbent assay (ELISA); the ability of NdBA to cross the blood-brain barrier (BBB) was also examined. The stage of cell cycle arrest was confirmed by using a fluorescence-activated cell-sorting (FACS) data analysis. Results: The average size of the nanoparticles was ~ 110 nm. Confocal microscopy images confirmed the presence of NdBA in the cellular cytoplasm. The bio-physical properties of dBA and NdBA ascertained from the CD and the Tm profiles revealed that NdBA had greater interaction with the target DNA than dBA did. Both dBA and NdBA arrested cell proliferation at G0/G1, NdBA showing the greater effect. NdBA also induced a greater degree of cytotoxicity in A549 cells, but it had an insignificant cytotoxic effect in normal L6 cells. The results of flow cytometric, cytogenetial and histopathological studies in mice revealed that NdBA caused less nuclear condensation and DNA damage than dBA did. TEM images showed the presence of NdBA in brain samples of NdBA fed mice, indicating its ability to cross the BBB. Conclusion: Thus, compared to dBA, NdBA appears to have greater chemoprotective potential against lung cancer.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.424.2-424.2
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• 2002

The in vivo release characteristics of rhGH-loaded PLGA microsphere prepared using a double emulsion process from hydrophilic 50:50 poly(D.L-lactide-co-glycolide) (PLGA) polymers were analyzed. This formulation showed particle size of ca 53.1$\mu\textrm{m}$ with high drug incorporation efficiency. To investigate in vivo release kinetics without the interference of formation of antibodies to rhGH in the experimental animals, the animals were immunosuppressed by treatment with Cyclosporin. (omitted)

• Polymer(Korea)
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• v.32 no.2
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• pp.143-149
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• 2008

We synthesized PEG-PLA (or PLGA) amphiphilic di-block copolymers, which consist of PEG as biocompatible and hydrophilic block and PLA (or PLGA) as biodegradable and hydrophobic block, by ring opening polymerization of LA in the presence of methoxy PEG as a macroinitiator. The compositions and the molecular weights of the copolymers were controlled by changing the feed ratio of LA (and GA) to PEG initiator. The di-block copolymers could self-assemble in aqueous media to form micellar structure. A hydrophobic model drug, pioglitazone, was loaded into the polymer micelle using solid dispersion and dialysis methods, and the drug-loaded micelles were characterized by AFM, DLS and HPLC measurements. The drug loading capacity and in vitro release studies were performed and evaluated under various conditions. These results indicated that the amphiphilic di-block copolymers of PEG-PLA (or PLGA) could solubilize pioglitazone by solid dispersion method and the drug release was modulated according to micellar chemical compositions.

• Polymer(Korea)
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• v.27 no.3
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• pp.226-234
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• 2003

Ipriflavone (IP), a non-hormonal isoflavone derivative, has been shown to interfere with bone remodeling by inhibiting bone resorption and stimulating bone formation. IP consistently increased the amount of Ca incorporated into the cell layer by mesenchymal stem cells (MSCs). In this study, we developed the novel IP loaded poly(L-lactide-co-glycolide) (PLGA) scaffolds for the possibility of the application of the tissue engineered bone. IP/PLGA scaffo1ds were prepared by solvent casting/salt leaching method and were characterized by porosimeter, scanning electron microscopy, determination of residual salt amount, differential scanning calorimetry, and X-ray diffractometer, respectively. IP/PLGA scaffolds were implanted into the back of athymic nude mouse to observe the effect of IP on the osteoinduction compared with control PLGA scaffo1ds. Thin sections were cut from paraffin embedded tissues and histological sections were stained H&E, von Kossa, and immunohistochemical staining for Type I collagen and osteocalcin. It can be observed that the porosity was above 91.7% and the pore size was above 101 $\mu\textrm{m}$. Control scaffo1d and IP/PLGA scaffo1ds of 50% IP were implanted on the back of athymic nude mouse to observe the effect of IP on the induction of cells proliferation for 9 weeks. The evidence of calcification, osteoblast, and osteoid from the undifferentiated stem cells in the subcutaneous sites and other soft connective tissue sites having a preponderance of stem cells has been observed. From these results, it seems that IP plays an important role for bone induction in IP/PLCA scaffolds.