• 폴리머
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• 제28권4호
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• pp.335-343
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• 2004

카뮤스틴 (1,3-bis(2-chloroethy1-nitrosourea, BICNU)은 뇌종양 치료를 위하여 임상적으로 사용되는 약물로 짧은 생물학적 반감기를 가지고 있어 장기방출에 적합하지 않다. 하지만, poly(D,L-lactide-co-glycolide) (PLGA)는 벌크 분해 특성으로 인해 약물의 장기방출에 유용하며, PLGA의 유도체인 글리콜라이드 단량체는 독성이 없고 PLGA와 유사한 생분해성을 가지고 있어 BICNU의 방출조절에 이용된다. 이 실험에서 BICNU를 함유한 PLGA 웨이퍼는 일반적인 직접압축법에 의해 제조한 후 BICNU의 방출거동과 웨이펴의 분해속도를 전자주사현미경, 핵자기공명장치 그리고 젤투과크로마토그래피를 통해 관찰하였다. 또한, 글리콜라이드 단량체의 함량변화에 따른 다중층 웨이퍼를 제조하여 단일층 웨이퍼와의 방출거동을 비교하였다. 이러한 결과들로부터 BICNU를 함유한 PLGA 웨이퍼의 약물방출은 BICNU와 글리콜라이드 단량체의 함량이 증가할수록 증가하였고, 다중층 웨이퍼에서 외부층의 글리콜라이드 단량체와 BICNU가 약물방출 거동과 분해속도에 영향을 미친다는 것을 확인하였다.

• 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.

• 한국염색가공학회지
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• 제10권5호
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• pp.32-38
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• 1998

Glycolides were polymerized by PPG or Pluronic(PN) to give A-B-A block copolyesters consisting of polyglycolide(A) and polypropylene glycol(B) or polyglycolide(A) and PN (B). Lactones were easily copolymerized with polyethers by ester interchange reaction even in the absence of catalyst. It is because PPG and PN are telechelic polyethers having hydroxy groups on their both ends. When the feed ratio of PPG(M$_{n}$=4,000) and PN(M$_{n}$=11,500) were over 5 and 10 wt% .elative to glycolide, respectively, the polymerization of glycolide took place from the terminus hydroxy groups of PPG or PN to produce the desired A-B-A block copolymers in high yields. The molecular weights of the copolymers, which estimated from the monomer conversions and the feed ratios of PPG and PN, could be controlled by changing the kind of terminus hydroxy of polyether and the feed molar ratio of PPG and PN. PN.

• 대한의용생체공학회:의공학회지
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• 제13권2호
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• pp.147-154
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• 1992

Poly (glycolic aclu-co-glycine-L-lactic aclu) has been prepared by rlng opening polymerlzation. The monomer 6-methyl morpholine-2, 5-dlone was synthe-slzed by bromoproplonylation of 2 bromopropionyl bromide with glycine. Glycolide and 6-methyl morpholine-2, 5-dione have been used as starling materials for polydepsipeptides. The synthesized copolymers have been Identlrled by NMR and FT-lR spectrophotometer. The Tg value of poly(glycollc aclu-co glycine-L-tactic acld ) Is In creased with increasing mole fraction of 6-methylmorpholine-2, 5-dlone(60-$84^{\circ}C$). The glass trasltion temperature of poly(glycolic acid-co-glycine-L-lactic-acid) (62-$86^{\circ}C$) is lower than that of poly (L-lactic acrid-co-glycine-L-lactic acid ). The thermal degradation of poly( L-lactic acid-co- glycine-L-lactic acid ) Is decreased with increasing mole fraction of L-lactide. The thermal degrada pion of poly(glycolic acrid-co-91ycine-L-lactic aclu ) is increased with increasing mole Fraction of glycolide.

• Korean Chemical Engineering Research
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• 제46권2호
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• pp.205-210
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• 2008

PLGA는 생분해성 고분자이며 생체적합성을 갖는 고분자로서 약물전달을 위한 연구에 많이 이용되고 있는 고분자이다. 그러나 PLGA를 약물전달에 이용할 때 약물의 급격한 초기방출 이후에 일정기간동안 약물이 방출되지 않는 지연시간이 존재하게 된다. 이러한 문제를 해결하기 위하여 PLGA 웨이퍼에 단량체를 첨가하여 제조하였다. 또한 PLGA를 재결정하여 약물의 급격한 방출 현상을 억제하도록 하였다. SEM을 이용하여 재결정된 PLGA의 형태학적 차이를 관찰하였으며 생체외 약물 방출거동은 HPLC를 이용하여 측정하였다. PLGA의 분해과정에서 단량체의 영향을 알아보기 위하여 GPC를 이용하여 분자량 변화를 측정하였다. 본 연구를 통하여 PLGA의 벌크분해에 기인한 지연시간을 없앨 수 있었으며 약물의 방출 기간을 3일까지 앞당길 수 있었다.

• 폴리머
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• 제30권6호
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• pp.464-470
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• 2006

메톡시 폴리(에틸렌 글리콜)(MPEG)과 생분해성 폴리에스테르 계열의 폴리카프로락톤(PCL), 폴리발레로락톤(PVL), 폴리락타이드(PLLA) 및 폴리 (락타이드-co-글리콜라이드) 공중합체(PLGA)로 이루어진 블록공중합체의 합성 및 특성을 비교하였다. MPEG-PCL과 MPEG-PVL 블록공중합체는 단량체 활성화제로서 $HCl{\cdot}Et_2O$의 존재 하에 상온에서 카프로락톤(${\epsilon}-CL$)과 발레로락톤(${\delta}-VL$)의 개환중합에 의해 합성하였으며, MPEG-PLLA와 MPEG-PLGA 블록공중합체는 $Sn(Oct)_2$의 존재 하에 $130^{\circ}C$에서 락타이드(L-LA)와 PLGA의 개환중합에 의해 합성하였다. 합성된 블록공중합체는 $^1H-NMR$, GPC, DSC 및 XRD의 측정을 통해 특성을 분석하였다. 합성된 NPEG-폴리에스테르 블록공중합체의 수용액 상에서의 미셀 특성은 $^1H-NMR$, 광산란기, 원자 현미경 및 형광 측정기를 이용하여 확인하였다. 원자 현미경을 통해 관찰된 미셀의 형태는 대부분의 블록공중합체에서 구형으로 존재함을 확인할 수 있었다. 본 연구에서는 미셀의 특성 비교를 통해 폴리에스테르 블록의 종류에 따라 열적 특성, 결정화도, 임계 미셀 농도 및 미셀의 직경이 다르게 나타남을 확인할 수 있었으며, MPEG-폴리에스테르 블록공중합체의 미셀내부에 선택적으로 소수성의 약물을 분포시킬 수 있으므로 소수성 약물 전달체로서의 가능성을 확인하였다.

• Macromolecular Research
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• 제11권4호
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• pp.207-223
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• 2003

For last five years, we are developing the novel local drug delivery devices using biodegradable polymers, especially polylactide (PLA) and poly(D,L-lactide-co-glycolide) (PLGA) due to its relatively good biocompatibility, easily controlled biodegradability, good processability and only FDA approved synthetic degradable polymers. The relationship between various kinds of drug [water soluble small molecule drugs: gentamicin sulfate (GS), fentanyl citrate (FC), BCNU, azidothymidine (AZT), pamidronate (ADP), $1,25(OH)_2$ vitamin $D_3$, water insoluble small molecule drugs: fentanyl, ipriflavone (IP) and nifedipine, and water soluble large peptide molecule drug: nerve growth factor (NGF), and Japanese encephalitis virus (JEV)], different types of geometrical devices [microspheres (MSs), microcapsule, nanoparticle, wafers, pellet, beads, multiple-layered beads, implants, fiber, scaffolds, and films], and pharmacological activity are proposed and discussed for the application of pharmaceutics and tissue engineering. Also, local drug delivery devices proposed in this work are introduced in view of preparation method, drug release behavior, biocompatibility, pharmacological effect, and animal studies. In conclusion, we can control the drug release profiles varying with the preparation, formulation and geometrical parameters. Moreover, any types of drug were successfully applicable to achieve linear sustained release from short period ($1{\sim}3$ days) to long period (over 2 months). It is very important to design a suitable formulation for the wanting period of bioactive molecules loaded in biodegradable polymers for the local delivery of drug. The drug release is affected by many factors such as hydrophilicity of drug, electric charge of drug, drug loading amount, polymer molecular weight, the monomer composition, the size of implants, the applied fabrication techniques, and so on. It is well known that the commercialization of new drug needs a lot of cost of money (average: over 10 million US dollar per one drug) and time (average: above 9 years) whereas the development of DDS and high effective generic drug might be need relatively low investment with a short time period. Also, one core technology of DDS can be applicable to many drugs for the market needs. From these reasons, the DDS research on potent generic drugs might be suitable for less risk and high return.