• 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.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.

• Journal of Periodontal and Implant Science
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• v.29 no.1
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• pp.193-207
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• 1999

The purpose of this study was to compare the clinical results of guided tissue regeneration(GTR) using a resorbable barrier manufactured from an copolymer of polylactic acid (PLA) and polylaetic-glycolic acid(PLGA) with those of nonresorbable ePTFE barrier. Thirty two patients(25 to 59 years old) with one radiographically evident intrabony lesion of probing depth ${\geq}$6mm participated in a 6-month controlled clinical trial. The subjects were randomly divided into three independent groups. The first group(n=8) received a ePTFE barrier. The second group (n=12) received a resorbable PLA/PLGA barrier. The third group (n=12) received a resorbable PLA/PLGA barrier combined with an alloplastic bone graft. Plaque index (PI), gingival index(GI), probing depth(PD), gingival recession, clinical attachment level(CAL), and tooth mobility were recorded prior to surgery and at 3, 6 months postsurgery, Statistical tests used to analyze these data included independent t-test, paired t-test, one-way ANOVA. The results were as follows : 1. Probing depth was significantly reduced in all groups at 3, 6 months postsurgery and there were not significant differences between groups. 2. Clinical attachment level was significantly increased in all groups at 3, 6 months postsurgery and there were not significant differences between groups. 3. There were not significant differences in probing depth, clinical attachment level, gingival recession, tooth mobility between second group (PLA/PLGA barrier) and third group (PLA/PLGA barrier combined with alloplastic bone graft) 4. Tooth mobility was not significantly increased in all groups at 3, 6 months postsurgery and there were not significant differences between groups. In conclusion, PLA/PLGA resorbable barrier has similar clinical potential to eP'IFE barrier in GTR procedure of intrabony pockets under the present protocol.

• Polymer(Korea)
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• v.24 no.4
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• pp.505-512
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• 2000

The mixture density data for poly(lactide-co-glycolide) [PLGA] with supercritical $CO_2$, CHF$_3$ and CHClF$_2$ were obtained in the temperature range of 27 to 10$0^{\circ}C$ and at pressures as high as 3000 bar (PLGA$_{x}$, Where the molar concentration of glycolide in the backbone, x, range from 0 to 50 mol%). The PLA-$CO_2$, PLA-CHF$_3$, and PLA-CHClF$_2$ systems dissolve in the pressure less than 1430 below 700, and below 100 bar, respectively. The mixture density shows from 1.084 to 1.334 g/cm$^3$ at temperatures from 27 to 93$^{\circ}C$. The PLGA$_{15}$ -$CO_2$ mixture dissolves at pressures of below 1900 bar and the mixture density is in the range of 1.158 to 1.247 g/cm$^3$ at temperatures between 37 and 92$^{\circ}C$. The solubilities of the PLGA$_{25}$ for $CO_2$, CHF$_3$, and CHClF$_2$ are shown to pressure as high as 2390, 1470, and 118 bar, respectively, and the mixture density exhibits iron 1.154 to 1.535 g/cm$^3$ at temperatures from 29 to 81$^{\circ}C$. The PLGA$_{50}$-$CO_2$ system does not dissolve at 24$0^{\circ}C$ and 3000 bar while the PLGA$_{50}$-CHCIF$_2$ does easily at 5$0^{\circ}C$ and 100 bar. The mixture density for the PLGA-CHClF$_2$ system increases even at low pressures as the glycolide molar concentration increases.es.es.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.5
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• pp.1725-1728
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• 2015

Objective: To explore effects of paclitaxel-loaded poly lactic-co-glycolic acid (PLGA) particles on the viability of human hepatocellular carcinoma (HCC) HepG2 cells. Materials and Methods: The viability of HepG2 cells was assessed using MTT under different concentrations of prepared paclitaxel-loaded particles and paclitaxel (6.25, 12.5, 25, 50, and 100 mg/L), and apoptosis was analyzed using Hochest33342/Annexin V-FITC/PI combined with an IN Cell Analyzer 2000. Results: Paxlitaxel-loaded nanoparticles were characterized by narrow particle size distribution (158.6 nm average particle size). The survival rate of HepG2 cells exposed to paclitaxel-loaded PLGA particles decreased with the increase of concentration and time period (P<0.01 or P<0.05), the dose- and time-dependence indicating sustained release (P<0.05). Moreover, apoptosis of HepG2 cells was induced, again with an obvious dose- and time-effect relationship (P<0.05). Conclusions: Paclitaxel-loaded PLGA particles can inhibit the proliferation and induce the apoptosis of HCC HepG2 cells. This new-type of paclitaxel carrier body is easily made and has low cost, good nanoparticle characterization and sustained release. Hence, paclitaxel-loaded PLGA particles deserve to be widely popularized in the clinic.

• Polymer(Korea)
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• v.24 no.6
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• pp.877-885
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• 2000

PLA, PGA and PLGA films were treated with chloric acid mixture solution [70% perchloric acid (HClO$_4$)/potassium chlorate (KClO$_3$) aq. saturated solution, 3 : 2] to increase surface wettability and thus cell compatibility. The surface-treated PLA, PGA, and PLGA films were characterized by the measurement of water contact angle, electron spectroscopy for chemical analysis, and scanning electron microscopy. Surface wettability of chloric acid-treated PLA, PGA, and PLGA film surfaces was gradually increased with increase of treatment time. Unlike EtOH pre-treatment, chloric acid-treated polymer films maintain hydrophilic surface after drying. In cell adhesion test, fibroblasts were cultured on the chloric acid-treated film surfaces for 1 and 2 days. As the surface wettability increased, the cell adhesion on the surface were increased. In conclusion, this study demonstrated that the surface wettability of polymer plays an important role for cell adhesion and proliferation behavior.

• YAKHAK HOEJI
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• v.45 no.6
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• pp.623-633
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• 2001

Various bupivacaine-loaded microspheres were prepared using poly(d,1-lactide) (PLA) and poly(d,1-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. The effects of process conditions such as drug loading, polymer type and solvent type on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency and yield of PLGA micro- spheres were higher than those of PLA microspheres. The prepared microspheres had an average particle size below 5${\mu}{\textrm}{m}$. The particle size range of microspheres was 1.65~2.24${\mu}{\textrm}{m}$. As a result of SEM, the particle size of PLA microspheres was smaller than that of PLGA microspheres. In morphology studies, microspheres showed a spherical shape and smooth surface in all process conditions. In thermal analysis, bupivacaine-loaded microspheres showed no peaks originating from bupivacaine. This suggested that bupivacaine base was molecular-dispersed in the polymer matrix of microspheres. The release pattern of the drug from microspheres was evaluated for 96 hours. The initial burst release of bupivacaine base decreased with increasing the molecular weight of PLGA, and the drug from microspheres released slowly. In conclusion, bupivacaine-loaded microspheres were successfully prepared from poly(d,1-lactide) and poly (d,1- lactic-co-glycolide) polymers with different molecular weights allowing control of the release rate.

• Journal of Biomedical Engineering Research
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• v.41 no.1
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• pp.62-66
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• 2020

Controlled drug release is important for effective treatment of cancer. Poly(DL-lactide-co-glycolide) acid (PLGA) is a Food and Drug Administration (FDA) approved polymer and have been extensively studied as drug delivery carriers with biodegradable and biocompatible properties. However, PLGA drug delivery carriers are limited due to the initial burst release of drug. Certain drugs require an early rapid release, but in many cases the initial rapid release can be inefficient, reducing therapeutic effects and also increasing side effects. Therefore, sustained release is important for effective treatment. Poly Lactic Acid stereo complex (PLA SC) is resistant to hydrolysis and has high stability in aqueous solutions. Therefore, in this work, PLGA based discoidal polymeric particles are modified by Poly Lactic Acid stereocomplex (PLAsc DPPs). PLAsc DPPs are 3 ㎛ in diameter, also showing a relatively sustained release profile. Fluorescein 5(6)-isothiocyanate (FITC) released from PLAsc DPPs was continuously observed until 38 days, which showed the initial release of FITC from PLAsc DPPs was about 3.9-fold reduced as compared to PLGA based DPPs at 1 hour.

• Polymer(Korea)
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• v.28 no.5
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• pp.382-390
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• 2004

One of the significant natural bioactive materials is demineralized bone particle (DBP) whose has a powerful induce. of new bone growth. In this study, we developed the DBP loaded poly-lactide (PLA) and poly(L-lactide-co-glycolide) (PLGA) scaffolds for the possibility of the application of the tissue engineered bone. PLA/DBP and PLGA/DBP scaffolds were prepared by solvent casting/salt leaching method and were characterized by porosimeter, scanning electron microscopy. BMSCs were stimulated by osteogenic medium and characterized by histological stained Wright-Giemsa, Alizarin red, von Kossa, and alkaline phosphate activity (ALP). DBP impregnated scaffolds with BMSCs were implanted into the back of athymic nude mouse to observe the effect of DBP on the osteoinduction compared with control scaffolds. It can be observed that the porosity was above $90.2\%$ and the pore size was above 69.1$\mu$m. BMSCs could be differentiated into osteoprogenitor cells as result of wright-giemsa, alizarin red, von Kossa and ALP staining. In in vivo study, we could observed calcification region in PLA/DBP and PLGA/DBP groups, but calcification did not occur almost in control scaffolds. From these results, it seems that DBP as well as BMSCs play an important role for bone induction in PLA/DBP and PLGA/DBP scaffolds.

• YAKHAK HOEJI
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• v.44 no.6
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• pp.511-520
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• 2000

Various bupivacaine-loaded microspheres were prepared from poly (d,l-lactide) (PLA) or poly (d,l-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. PLA and PLGA microspheres were prepared by w/o/w and w/o/o multiple emulsion solvent evaporation, respectively. The effects of process conditions such as emulsification speed, emulsifier type, emulsifier concentration and internal/external phase ratio on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency was higher in the microspheres prepared by w/o/o multiple emulsion than that by w/o/w multiple emulsion method, because the solubility of bupivacaine HCI was decreased in oil phase compared with water phase. The prepared microspheres had an average diameter between 1 and $2\;{\mu}M$ in all conditions of two methods. In morphology studies the PLA microspheres showed an irregular shape and smooth surface, but PLGA microspheres had a spherical shape and smooth surface. The release pattern of the drug from microspheres was evaluated on the basis of the burst effect and the extent of the release after 24h. The in vitro release of bupivacaine HCl from microspheres showed a large initial burst release and $60{\sim}80%$ release within one day in all conditions of two methods. The extents of the burst release against PLA and PLGA microspheres were $30{\sim}50%$ and $50{\sim}80%$ within 20min, respectively. This burst release seems to be due to the smaller size of microspheres and the solubility of drug in water.