• 약학회지
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• 제44권4호
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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.

• 폴리머
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• 제32권2호
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• pp.143-149
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• 2008

생체적합성을 가진 친수성 poly(ethylene glycol)(PEG)블록과 생분해성 고분자인 Poly(D,L-lactide)(PLA) 또는 poly(lactide-co-glycolide)(PLGA)를 소수성 블록으로 하는 양친성 이중 블록공중합체를 합성하여 난용성 당뇨병 치료제인 pioglitazone의 가용화를 위한 고분자 미셀을 제조하였다. PEG 말단으로부터 LA의 개환중합에 의해 합성된 고분자의 화학적 조성과 분자량은 반응액 내 당량비로 조절하였고, 합성된 고분자는 수용액 상에서 $10{\sim}30\;nm$ 크기인 구형의 자기조립 미셀을 형성하였다($CMC=0.001{\sim}0.0076\;mg/mL$). 투석법과 고체분산법을 이용하여 약물을 봉입한 후 AFM, DLS, HPLC 분석을 통하여 미셀의 특성을 비교하였다. 결론적으로 PEG-PLA(또는 PLGA) 공중합체를 이용한 고체분산법을 통해 pioglitazone을 효과적으로 가용화시킬 수 있었다.

• Journal of Periodontal and Implant Science
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• 제29권1호
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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.

• 폴리머
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• 제24권4호
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• pp.505-512
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• 2000

본 연구는 초임계 용매인 $CO_2$, CHF$_3$ 및 CHClF$_2$내에서 poly(lactide-co-glycolide) [PLGAI 용액과의 흔합물 밀도를 측정하였다. 초임계 용매와 Poly(lactic acid) [PLA] 및 PLGA간의 흔합물 밀도는 온도 27-10$0^{\circ}C$와 압력 3000 bar까지 실험하여 나타내었다 [PLGA$_{x}$의 X는 0~50 mo1% 범위에 대한 glycolide의 몰농도이다]. PLA-$CO_2$ 흔합물은 약 1430 bar 이내에서, PLA-CHF$_3$계는 700 bar 이하에서, PLA-CHClF$_2$계는 100bar 이하에서 각각 용해되었다. 이때 온도범위는 27~93$^{\circ}C$이며, 흔합물 밀도는 1.084~l.334g/$cm^3$ 범위에서 나타났다. PLGA$_{15}$ 공중합체-$CO_2$ 흔합물은 약 1900 bar 이하에서 용해되었으며, 이때 혼합물 밀도는 37~92$^{\circ}C$에서 1.158~l.247g/$cm^3$으로 나타났다. PLGA$_{25}$공중합체-$CO_2$계는 약 2390 bar이하에서, PLGA$_{25}$-CHF$_3$계에 대해서는 1470 bar이하에서, PLGA$_{25}$-CHClF$_2$계에 대해서는 118 bar 이하에서 각각 용해되었으며, 흔합물 밀도는 29~81$^{\circ}C$사이에서 1.154~1.535g/$cm^3$로 나타났다. PLGA$_{50}$-$CO_2$계는 24$0^{\circ}C$, 3000 bar내fl서는 용해되지 않았으며, 반면 PLGA$_{50}$과 CHClF$_2$의 흔합물은 오히려 5$0^{\circ}C$와 100 bar내에서 쉽게 용해되었다. 또한 PLGA와 CHClF$_2$계는 glycolide 농도가 증가함에 따라 흔합물 밀도가 증가하였다.다..다..다..

• Asian Pacific Journal of Cancer Prevention
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• 제16권5호
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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.

• 폴리머
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• 제24권6호
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• pp.877-885
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• 2000

본 연구에서는 폴리락타이드 (PLA), 폴리글리콜라이드 (PGA) 그리고 이들의 공중합체인 PLGA 필름을 염소산 혼합용액 [70% 과염소산 (HClO$_4$)/포타슘 클로레이트 (KClO$_3$) 포화 수용액, 3 : 2]으로 처리하여 표면의 젖음성과 세포적합성을 증가시켰다. 표면 처리된 고분자의 표면을 물접촉각 측정과 ESCA, SEM으로 특성결정하였다. 염소산 처리된 PLA, PGA, 및 PLGA의 표면 젖음성은 처리시간이 증가함에 따라 증가되었고 이들 고분자 필름은 기존의 에탄을 전처리와 달리 건조 후에도 친수성 표면을 유지하였다. 세포 점착실험은 섬유아세포를 염소산 처리된 필름의 표면에서 1일 및 2일 배양하였고 표면의 젖음성이 증가함에 따라 세포의 점착도 우세하였다. 결론적으로 본 연구에서는 표면의 젖음성은 세포의 점착과 증식 거동에 중요한 역할을 한다는 것을 증명하였다.

• 약학회지
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• 제45권6호
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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.

• 대한의용생체공학회:의공학회지
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• 제41권1호
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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.

• 폴리머
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• 제28권5호
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• pp.382-390
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• 2004

생체적합성 천연재료 중 하나인 탈미네랄화된 골분 (demineralized bone particle, DBP)은 골형성단백질 (BMP)을 함유하고 있어 골수간엽줄기세포 (BMSCs)의 분화를 유도한다. 본 연구에서는 DBP를 함유한 폴리 락타이드 (PLA)와 락타이드-글리콜라이드 공중합체 (PLGA) 다공성 지지체를 용매 캐스팅/염추출법으로 제조하였고, 수은다공측정계 및 전자주사현미경을 이용하여 특성결정 하였다. BMSCs는 골분화 배지를 이용하여 조골세포로 분화시켜 Wright-Giemsa, Alizarin red, von Kossa 및 ALP 염색으로 확인하였다. DBP가 함유된 지지체와 DBP가 함유되지 않은 지지체에 BMSCs를 파종한 후 면역결핍 누드마우스의 피하에 삽입하여 이들의 골형성 정도를 비교하여 보았다. 제조한 지지체의 다공도는 $90.2\%$ 이상이었고 평균 다공크기도 69.1$\mu$m 이상이었다. BMSCs는 Wright-Giemsa, Alizarin red, von Kossa 및 ALP 염색결과 조골세포로 분화가 가능했으며, 동물실험을 수행한 결과 DBP가 함유된 지지체에서 칼슘침착 영역을 확인할 수 있었지만 DBP가 함유되지 않은 지지체에서는 칼슘침착 영역을 확인하지 못하였다. 결론적으로 DBP를 함유한 지지체에서 DBP와 BMSCs가 골형성에 중요한 요인으로 작용한다고 사료된다.

• 약학회지
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• 제44권6호
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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.