• 제목/요약/키워드: Poly (lactide-co-glycolide)

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Poly(DL-lactide-co-glycolide) 공중합체의 합성과 그 응용 (I). Poly(DL-lactide-co-glycolide)(80:20) 공중합체를 이용한 Clonazepam의 방출특성 (Synthesis of Poly(DL-lactide-co-glycolide) Copolymers and Its Application (I). Release Characteristics of Clonazepam Using Poly(DL-lactide-co-glycolide) (80:20) Copolymers)

  • 나재운;이동병;조종수;정영일;김성호;김성현
    • 대한화학회지
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    • 제42권1호
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    • pp.92-98
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    • 1998
  • DL-lactide와 glycolide로부터 공중합체 Poly(DL-lactide-co-glycolide)(80:20)를 합성하였다. 합성된 공중합체에 소수성 약물인 clonazepam을 함유하는 미소구체를 제조하여 약물전달시스템 제제로서 응용 가능성을 고찰하였다. 미소구체로부터 약물방출실험은 pH 7.4 phosphate buffer solution $37.0{\pm}0.05^{\circ}C$에서 시행하였다. 미소구체로부터 약물이 선형적으로 방출된 시간범위는 고분자와 약물의 무게비가 20:40(mg)인 경우는 51일 이었고, 20:20과 40:20 (mg)의 비율의 경우는 각각 41일, 29일로 미소구체 제조시 약물의 비율이 증가함에 따라 방출시간 또 한 길어짐을 알 수 있다. 결론적으로 본 실험의 diafiltration법에 의해 균일한 크기의 미소구체를 제조할 수 있었으며, 약물은 조절 방출형 pattern을 보여 약물전달시스템 제제로의 응용 가능성을 알 수 있었다.

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Effect of pH on the Formation of Acylated Octreotides by Poly(lactide-co-glycolide)

  • Na, Dong-Hee
    • Journal of Pharmaceutical Investigation
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    • 제40권4호
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    • pp.251-254
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    • 2010
  • The formation of acylated peptide impurities in poly(lactide-co-glycolide) (PLGA) formulations is one of the major challenges to the development of successful sustained-release product. Octreotide, synthetic analogue of somatostatin, has been identified to be acylated in PLGA microsphere formulations. The purpose of this study was to investigate the pH effect on the formation of acylated octreotides by PLGA. In the incubation with PLGA in 0.1 M phosphate buffer at pH 7.4, approximately 98% of octreotide adsorbed to PLGA through 14 days and 66.3% of acylated octreotides were produced after 42 days, whereas the interaction of octreotide with PLGA was significantly inhibited in the incubation at pH 4, in which the acylated octreotides were observed to be 9.2% after 42 days. In the interaction study at pH 4.1-7.4, the production of acylated octreotides was demonstrated to be dependent on environmental pH. Below pH 5.0, the acylation of octreotide was significantly inhibited. This study indicates that the pH is the major factor for the formation of acylated octreotide in PLGA formulations.

계면활성제를 사용하지 않는 Poly(DL-lactide-co-glycolide) 나노입자로부터의 Norfloxacin 방출과 생분해 특성 (Norfloxacin Release from Surfactant-Free Nanoparticles of Poly(DL-lactide-co-glycolide) and Biodegradation)

  • 권중근;정영일;장미경;이창형;나재운
    • 폴리머
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    • 제26권4호
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    • pp.535-542
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    • 2002
  • 투석법을 이ctide-co-glycolide) (PLGA) 나노입자를 제조하고 다양한 용매에 따른 입자 크기, 약물 함유량, 생분해도 등과 같은 물리ㆍ화학적 특성을 조사하였다. Dimethylacetamide (DMAc), dimethylformamide (DMF), dimethylsulfoxide (DMSO)로 제조된 PLGA 나노입자의 크기는 acetone으로 제조한 입자보다 적었다. 또한, 약물 함유량은 DMAc>DMF>DMSO=acetone 순서였다. PLGA 나노입자는 scanning electron microscopy (SEM)과 transmission electron microscopy (TEM)의 측정으로 구형임을 알 수 있었다. 계면활성제를 사용하지 않는 나노입자에 봉입된 norfloxacin (NFx)은 X-ray diffraction 분석을 통하여 입자 표면에 약물을 가지지 않는 좋은 약물 봉입 효율을 가짐을 알 수 있었다. 모델약물로 사용된 NFx의 방출속도는 약물 함유량뿐만 아니라 입사크기에 의해 좌우된다. 또한 PLGA 나노입자의 분해속도는 아세톤보다는 DMF를 사용하였을 때 더 빠르며 이는 PLGA 나노입자의 생분해성도 입자크기에 좌우된다는 것을 알 수 있었다.

생체분해성 Poly(glycolide-co-ε-caprolactone-co-L-lactide) 블록 공중합물의 비등온 결정화 거동에 관한 연구 (Non-isothermal Crystallization Behavior of Poly(glycolide-co-ε-caprolactone-co-L-lactide) Block Copolymer)

  • 최세영;송승호
    • Elastomers and Composites
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    • 제49권1호
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    • pp.13-23
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    • 2014
  • 본 연구에서는 생체분해성 폴리에스터 계열의 glycolide, L-lactide 및 ${\varepsilon}$-caprolactone 단량체를 이용하여 2단계 중합법에 의한 삼원 공중합체를 제조하여, DSC를 이용한 비등온 결정화 거동을 고찰하였다. 보다 더 정확한 거동을 검토하기 위하여 Avrami 식과 Ozawa 식을 조합하여 비등온 결정화 거동을 고찰하였다. 과냉각도를 분석한 결과 PGCLA21의 값이 가장 큰 값을 보이고 있으며 L-lactide 함량이 증가함에 따라 과냉각도는 증가하는 경향을 보이고 있다. 수정된 Avrami 식을 이용하여 다양한 냉각속도에서 비등온 결정화 거동 결정화 속도 상수는 큰 경향을 보이고 있지 않는 것을 알 수 있었다. Avrami 및 Ozawa 식을 조합하여 특정한 상대적 결정화도에서의 냉각함수를 구한결과 L-lactide 함량이 증가하면서 PGCL과 비교시 결정화 속도를 향상시키는 역할을 하고 있는 것으로 여겨지는 반면 PGCLA41과 PGCLA21을 비교시 L-lactide 함량이 일정 이상 증가시 logF(T) 값이 큰 것을 확인 할 수 있는데 이는 동일한 결정을 얻는데 더 많은 냉각 속도를 필요로 한다는 것을 의미하며 결정화 속도 향상에 부정적인 영향을 미치는 것으로 판단된다.

용매증발법에 의한 부피바카인 마이크로스피어의 제조 및 평가 (II) (Preparation and Evaluation of Bupivacaine Microspheres by a Solvent Evaporation Method (II))

  • 곽손혁;이시범;이종수;이병철;황성주
    • 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.

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Core-shell Poly(D,L-lactide-co-glycolide )/Poly(ethyl 2-cyanoacrylate) Microparticles with Doxorubicin to Reduce Initial Burst Release

  • Lee, Sang-Hyuk;Baek, Hyon-Ho;Kim, Jung-Hyun;Choi, Sung--Wook
    • Macromolecular Research
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    • 제17권12호
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    • pp.1010-1014
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    • 2009
  • Monodispersed microparticles with a poly(D,L-lactide-co-glycolide) (PLGA) core and a poly(ethyl 2-cyanoacrylate) (PE2CA) shell were prepared by Shirasu porous glass (SPG) membrane emulsification to reduce the initial burst release of doxorubicin (DOX). Solution mixtures with different weight ratios of PLGA polymer and E2CA monomer were permeated under pressure through an SPG membrane with $1.9\;{\mu}m$ pore size into a continuous water phase with sodium lauryl sulfate as a surfactant. Core-shell structured microparticles were formed by the mechanism of anionic interfacial polymerization of E2CA and precipitation of both polymers. The average diameter of the resulting microparticles with various PLGA:E2CA ratios ranged from 1.42 to $2.73\;{\mu}m$. The morphology and core-shell structure of the microparticles were observed by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The DOX release profiles revealed that the microparticles with an equivalent PLGA:E2CA weight ratio of 1:1 exhibited the optimal condition to reduce the initial burst of DOX. The initial release rate of DOX was dependent on the PLGA:E2CA ratio, and was minimized at a 1:1 ratio.

poly(D,L-lactide-co-glycolide) nanoparticles제조와 약물방출 거동 및 생분해도

  • 유정준;정영일;오동석;임균택
    • 한국생물공학회:학술대회논문집
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    • 한국생물공학회 2000년도 춘계학술발표대회
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    • pp.550-553
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    • 2000
  • The polymeric matrices made with poly(D,L-lactide-co-glycolide) were prepared using copolymer of poly(D,L-lactide) and poly(ethylene glycol) for application of drug delivery systems. Catalyst made use of stannous actoate. Particle size were differ greatly$(435.3{\pm}11.2{\sim}2284.1{\pm}188.5)$ that nanoparticle made use of according to solvent of various kinds. Polymer could a sharp distinction with copolymerized among LE-1, LE-2 and LE-3 of PLA and PEG of content that to examine $^1H-NMR$ of copolymer make refine and reprecipitation. Drug delivery effect at PLGA nanoparticle : PLA amount more then proved highly drug delivery amount that each LE-1, LE-2, LE-3, drug and solvent was 40mg, 20mg and 10mg. Drug delivery effect proved higher 20mg that change(10mg, 20mg, 40mg) at drug feeding amount with LE-2. The first a lot of drug proved delivery. LE-3 most lactide content proved much delivery since biodegradable on PLGA copolymer result from lactide. Also biodegradable rate was highest at LE-3 much of lactide content, because influence at biodegradable effect of lactide by inclusive of soft PEG.

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경구용 항원 수송체 모델로서 폴리락티드-글리콜리드 마이크로스피어의 입자도 조절 (Particle Size Control of Poly(Lactide-co-Glycolide) Microspheres for Oral Antigen Delivery Systems)

  • 송일용;송세현;송우헌;조성완;최영욱
    • Journal of Pharmaceutical Investigation
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    • 제29권4호
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    • pp.315-321
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    • 1999
  • Poly (lactide-co-glycolide) (PLGA) microspheres containing ovalbumin (OVA) as a model protein drug were prepared by double emulsification method, and various conditions such as mixing rate, volume of outer phase and isopropyl alcohol concentration in outer phase during secondary emulsification were observed to control the size of microspheres. In addition, entrapment efficiency of OVA and protein denaturation were also evaluated. As the rate of stirring was increased, the size of particles was decreased. But excessive stirring increased the particle size of microspheres. In a preparation condition of small volume of outer phase, the particle size was decreased but the entrapment efficiency was increased. Adding isopropyl alcohol to outer phase decreased the size of particles, but increased the entrapment efficiency. Microparticles should have smaller size than $10\;{\mu}m$ to be uptaked by Peyer's patch in small intestine. High speed of mixing and relatively small volume of outer phase are needed to reduce the size. In addition, appropriate amount of isopropyl alcohol in outer phase also plays an important role in size reduction of PLGA microspheres.

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