• Title/Summary/Keyword: poly (lactide-co-glycolide)

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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 (Poly(DL-lactide-co-glycolide) 공중합체의 합성과 그 응용 (I). Poly(DL-lactide-co-glycolide)(80:20) 공중합체를 이용한 Clonazepam의 방출특성)

  • Nah, Jae Woon;Lee, Dong Byung;Cho, Chong Su;Jeong, Young Il;Kim, Sung Ho;Kim, Sung Hyun
    • Journal of the Korean Chemical Society
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    • v.42 no.1
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    • pp.92-98
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    • 1998
  • Poly(DL-lactide-co-glycolide) (80:20) was synthesized from DL-lactide and glycolide, and the copolymers was made to micelles containing clonazepam for drug delivery system. The release experiments of the drug from micelles were operated at pH 7.4 phosphate buffer solution $37.0{\pm}0.05^{\circ}C$. The linearly-releasing time ranges of the drug from micelles prepared with the copolymer/drug weight ratio of 20:40, 20:20, and 40:20 (mg) were 50, 41, and 29 days, respectively. So the linearly-releasing time of drug showed the order of micelles 20/40 > micelles 20/20 > micelles 40/20. In short, the formulation allows polymeric micelles to suppress the burst effect of the drug release mechanism, which led to the controlled release pattern and the possibility of drug delivery system for veinous injection.

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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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    • v.40 no.4
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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.

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

  • 권중근;정영일;장미경;이창형;나재운
    • Polymer(Korea)
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    • v.26 no.4
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    • pp.535-542
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    • 2002
  • We have prepared the surfactant-free nanoparticles of poly(DL-lactide-co-glycolide) (PLGA) by dialysis method and their physicochemical properties such as particle size and drug contents were investigated against various solvent. The size of PLGA nanoparticles prepared by using dimethylacetamide (DMAc), dimethylformamide (DMF), and dimethylsulfoxide (DMSO) was smaller than that from acetone. Also, the order of drug contents was DMAc>DMF>DMSO=acetone. These phenomena could be expected from the fact that solvent affects the size of nanoparticles and drug contents. The PLGA nanoparticles have a good spherical shapes as observed from scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Also, surfactant-free nanoparticles entrapping norfloxacin (NFx) have a good drug loading capacity without free-drug on the surface of nanoparticles confirmed by the analysis of X-ray powder diffraction. Release kinetics of NFx used as a model drug was governed not only by drug contents but also by particle size. Also, the biodegradation rate of PLGA nanoparticles prepared from DMF was faster than that prepared from acetone, indicating that the biodegradation of PLGA nanoparticles is size-dependent.

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

  • Choi, Sei-Young;Song, Seung-Ho
    • Elastomers and Composites
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    • v.49 no.1
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    • pp.13-23
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    • 2014
  • In this work, glycolide, L-lactide and ${\varepsilon}$-caprolactone monomers were polymerized into the triblock copolymers by two step polymerization method and their non-isothermal crystallization behaviors were studied by combination of modified Avrami and Ozawa formula for further analysis of their behaviors. The result showed that PGCLA21 gave the highest value for supercooling analysis and super cooling degree increased with L-lactide content. Crystallization velocity constant, however, showed no significant change. The result of cooling function in specific relative crystallization degree showed that the increase of L-lactide content made an effect on the more enhancement of crystallization velocity of the PGCLA than PGCL. The result of big logF(T) value with the L-lactide content above critical point for PGCLA41 and PGCLA21 showed that bigger cooling velocity needed to gain same crystal size compared with PGCL. This means that it gives negative effect in the increase of crystallization velocity.

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

  • 곽손혁;이시범;이종수;이병철;황성주
    • 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.

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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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    • v.17 no.12
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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

  • Yu, Jeong-Jun;Jeong, Yeong-Il;O, Dong-Seok;Im, Gyun-Taek
    • 한국생물공학회:학술대회논문집
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    • 2000.04a
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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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Particle Size Control of Poly(Lactide-co-Glycolide) Microspheres for Oral Antigen Delivery Systems (경구용 항원 수송체 모델로서 폴리락티드-글리콜리드 마이크로스피어의 입자도 조절)

  • Song, Il-Yong;Song, Seo-Hyun;Song, Woo-Heon;Cho, Seong-Wan;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.29 no.4
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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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