• 폴리머
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• 제31권1호
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• pp.20-24
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• 2007

제조과정에서 단백질 약물의 생물학적 활성의 보존은 약물의 성공적인 전달에 있어 여전히 중요한 과제이다. 이중에멀션 유기용매 증발법을 사용하여 나노입자를 제조하였고, 입자의 형태, 크기, 함입률 그리고 방출속도와 방출되는 효소의 활성을 살펴보았다. 입자의 크기는 고분자인 락타이드 글리콜라이드 공중합체의 농도가 증가할수록 커졌으며, 유화제의 농도에는 큰 차이가 없었으나, 4% PVA의 사용에서 가장 좁은 입자분포를 얻을 수 있었다. 최적의 조건에서 72.6%의 단백질 함입률과 $198.3{\pm}13.8 nm$ 크기의 나노입자를 얻었다. 입자로부터 효소의 방출은 첫 방출시기에 매우 빠르게 일어났으며 12일 내에 83%가 방출되었다. 이에 따른 방출되는 효소의 활성은 6일째까지 증가되었다.

• 폴리머
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• 제34권6호
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• pp.527-533
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• 2010

Pioglitazone을 봉입한 poly(lactide-co-glycolide)(PLGA) 나노입자를 emulsion-evaporation 방법을 이용하여 제조하여 최적의 나노입자와 봉입률을 조절하였다. 제조된 나노입자의 크기는 125~170 nm이었으며 30% pioglitazone이 봉입된 나노입자(3% PVA)의 봉입률은 85% 이상이었다. 이러한 나노입자들은 40일 동안 일정하게 용출이 되었다. 당뇨병 모델을 이용한 동물실험에서 글루코오스 농도를 저하시켰을 뿐만 아니라, 조직검사에서는 낮은 독성을 가지고 있는 것을 확인하였다. 이러한 결과는 pioglitazone 경구투여를 위한 약물전달을 위한 운반체로 사용될 수 있음을 확인하였다.

• 폴리머
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• 제34권3호
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• pp.274-281
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• 2010

본 실험에서는 일련의 poly(ethylene glycol)-poly(D,L-lactide)(또는 -poly(D,L-lactide-co-glycolide))이중블록 공중합체들을 D,L-lactide(또는 glycolide)의 고리열림 중합에 의해 합성하고, 당뇨병 치료제 일종인 rosiglitazone의 가용화를 위한 고분자 미셀 제형으로서의 특성을 평가하였다. 고체분산법을 이용하여 높은 봉입률의 약물함유 미셀 제형을 효과적으로 제조하였고, 미셀 제형의 수용액 내 안정성을 hydrotropic agent의 일종인 2-hydroxy-N-picolylnitinamide(HPNA)의 사용으로 더욱 향상시킬 수 있었다. 생체 외 세포생존평가에서 생체적합성과 낮은 독성을 보였고, 쥐를 이용한 동물실험에서도 약물을 함유한 고분자 미셀이 약물 대조군보다 혈당을 보다 효과적으로 감소시켰다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2008년도 Proceedings of the Convention
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• pp.164-164
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• 2008

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.268.2-269
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• 2000

• Macromolecular Research
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• 제16권8호
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• pp.717-724
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• 2008

In this study, we prepared all-trans retinoic acid (ATRA)-encapsulated, surfactant-free, PLGA nanoparticles. The nanoparticles were formed by nanoprecipitation process, after which the solvent was removed by solvent evaporation or dialysis method. When a nanoparticle was prepared by the nanoprecipitation - solvent evaporation method, the nanoparticles were bigger than the nanoparticles of the nanoprecipitation - dialysis method, despite the higher although loading efficiency. Nanoparticles from the nanoprecipitation - dialysis method were smaller than 200 nm in diameter, while the loading efficiency was not significantly changed. Especially, nanoparticles prepared from DMAc, 1,4-dioxane, and DMF had a diameter of less than 100 nm. In the transmission electron microscopy (TEM) observations, all of the nanoparticles showed spherical shapes. The loading efficiency of ATRA was higher than 90% (w/w) at all formulations with exception of THF. The drug content was increased with increasing drug-feeding amount while the loading efficiency was decreased. In the drug release study, an initial burst was observed for $2{\sim}6$ days according to the variations of the formulation, after which the drug was continuously released over one month. Nanoparticles from the nanoprecipitation - dialysis method showed faster drug release than those from the nanoprecipitation - solvent evaporation method. The decreased drug release kinetics was observed at lower drug contents. In the tumor cell cytotoxicity test, ATRA-encapsulated, surfactant-free, PLGA nanoparticles exhibited similar cytotoxicity with that of ATRA itself.

• Biomaterials and Biomechanics in Bioengineering
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• 제2권2호
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• pp.85-96
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• 2015

This study developed biodegradable bi-layered drug-eluting beads and investigated the in-vitro release of fluorouracil and cisplatin from the beads. To manufacture the drug-eluting beads, poly[(d,l)-lactide-co-glycolide] (PLGA) with lactide:glycolide ratios of 50:50 and 75:25 were mixed with fluorouracil or cisplatin. The mixture was compressed and sintered at $55^{\circ}C$ to form bi-layered beads. An elution method was employed to characterize the release characteristic of the pharmaceuticals over a 30-day period at $37^{\circ}C$. The influence of polymer type (i.e., 50:50 or 75:25 PLGA) and layer layout on the release characteristics was investigated. The experiment suggested that biodegradable beads released high concentrations of fluorouracil and cisplatin for more than 30 days. The 75:25 PLGA released the pharmaceuticals at a slower rate than the 50:50 PLGA. In addition, the bi-layered structure reduced the release rate of drugs from the core layer of the beads. By adopting the compression sintering technique, we will be able to manufacture biodegradable beads for long-term drug delivery of various anti-cancer pharmaceuticals.

• Journal of Pharmaceutical Investigation
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• 제31권3호
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• pp.191-196
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• 2001

Biodegradable polymeric microspheres were studied for their usefulness as carriers for the delivery of vaccine antigens. However, protein antigen could be denatured during microencapsulation processes due to the exposure to the organic phase and stress condition of cavitation and shear force. Therefore this study was carried out to re-evaluate the degree of protein denaturation during microencapsulation with poly(lactide-co-glycolide) (PLGA) copolymer. PLGA microspheres containing ovalbumin (OVA), prepared by W/O/W multiple emulsification method, were suspended in pH 7.4 PBS and incubated with shaking at $37.5^{\circ}C$. Drug released medium was collected periodically and analyzed for protein contents by micro-BCA protein assay. In order to evaluate the protein integrity, release medium was subjected to the analyses of SDS-PAGE and size exclusion chromatography (SEC). And enzyme-linked immunosorbent assay (ELISA) was introduced to measure the immunoreactivity of entrapped OVA and to get an insight into the three-dimensional structure of epitope. The structures of entrapped protein were not affected significantly by the results of SDS-PAGE and SEC. However, immunoreactivity of released antigen was varied, revealing the possibility of protein denaturation in some microspheres when it was evaluate by ELISA method. Therefore, in order to express the degree of protein denaturation, antigenicity ratio (AR) was obtained as follows: amount of immunoreactivity of OVA/total amount of OVA released ${\times}100(%)$. ELISA method was an efficient tool to detect a protein denaturation during microencapsulation and the comparison of AR values resulted in more accurate evaluation for immunoreactivity of entrapped protein.

• Macromolecular Research
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• 제11권3호
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• pp.183-188
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• 2003

The controlled delivery of anticancer agents using biodegradable polymeric implant has been developed to solve the problem of penetration of blood brain barrier and severe systemic toxicity. This study was performed to prepare 5-FU-loaded poly (L-lactide-co-glycolide) (PLGA) wafer fabricated microparticles prepared by two different method and to evaluate their release profile for the application of the treatment of brain tumor. 5-FU-loaded PLGA microparticles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). SEM observation of the 5-FU-loaded PLGA microparticles prepared by rotary solvent evaporation method showed that 5-FU was almost surrounded by PLGA and significant reduction of crystallinity of 5-FU was confirmed by XRD. In case of release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by mechanical mixing, the release profile of 5-FU followed near first order release kinetics. In contrast to the above result, release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by rotary solvent evaporation method followed near zero order release kinetics. These results indicate that preparation method of the 5-FU-loaded PLGA microparticles to fabricate into wafers was contributed to drug release profile.

• Korean Chemical Engineering Research
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• 제51권6호
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• pp.727-732
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• 2013

본 연구는 역오팔 지지체를 이용하여 인간지방유래 줄기세포의 연골 분화를 촉진하는 내용을 담고 있다. 비 다공성 구조를 가진 지지체에서 세포를 분화 시도하였을 경우 분화가 잘 촉진되지 않는 것에 비해 200 nm 정도의 균일한 구멍을 가지는 poly(D,L-lactide-co-glycolide)로 구성된 역오팔 지지체는 그 다공성 구조로 인하여 지지체의 내부까지 산소와 유기물의 수송을 가능하게 하여 지지체 내에서 어떤 유전적, 약물적 처리 없이 인간지방유래 줄기세포가 분화가 잘 되게 하는 것을 확인하였다.