• Bulletin of the Korean Chemical Society
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• 제33권10호
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• pp.3225-3232
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• 2012

The purposes of this research were to synthesize amoxicillin-carrying magnetic nanoparticles. Magnetic nanoparticles were prepared by a chemical precipitation of ferric and ferrous chloride salts in the presence of a strong basic solution. PLGA and PLGA-PEG copolymers were prepared by ring opening polymerization of lactide (LA) and glycolide (GA) (mole ratio of LA: GA 3:1) with or without polyethylene glycol (PEG). Amoxicillin loaded magnetic PLGA and PLGA-PEG nanoparticles were prepared by an emulsion-evaporation process (o/w). Transmission electron microscopy (TEM) and scanning electron microscopy (SEM) photomicrographs showed that the magnetic nanoparticles have the mean diameter within the range of 65-260 nm also they were almost spherical in shape. Magnetic nanoparticles prepared with PLGA showed more efficient entrapment (90%) as compared with PLGA-PEG (48-52%) nanoparticles. In-vitro release of amoxicillin from magnetic PLGA nanoparticles showed that 78% of drug was released over 24 hours. The amount of amoxicillin released from PLGA-PEG s was higher than PLGA.

• 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.

• Asian Pacific Journal of Cancer Prevention
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• 제16권18호
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• pp.8259-8263
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• 2016

Background: Nano-therapy has the potential to revolutionize cancer therapy. Chrysin, a natural flavonoid, was recently recognized as having important biological roles in chemical defenses and nitrogen fixation, with anti-inflammatory and anti-oxidant effects but the poor water solubility of flavonoids limitstheir bioavailability and biomedical applications. Objective: Chrysin loaded PLGA-PEG-PLGA was assessed for improvement of solubility, drug tolerance and adverse effects and accumulation in a gastric cancer cell line (AGS). Materials and Methods: Chrysin loaded PLGA-PEG copolymers were prepared using the double emulsion method (W/O/W). The morphology and size distributions of the prepared PLGA-PEG nanospheres were investigated by 1H NMR, FT-IR and SEM. The in vitro cytotoxicity of pure and nano-chrysin was tested by MTT assay and miR-34a was measured by real-time PCR. Results: 1H NMR, FT-IR and SEM confirmed the PLGA-PEG structure and chrysin loaded on nanoparticles. The MTT results for different concentrations of chrysin at different times for the treatment of AGS cell line showed IC50 values of 68.2, 56.2 and $42.3{\mu}M$ and 58.2, 44.2, $36.8{\mu}M$ after 24, 48, and 72 hours of treatment, respectively for chrysin itslef and chrysin-loaded nanoparticles. The results of real time PCR showed that expression of miR-34a was upregulated to a greater extent via nano chrysin rather than free chrysin. Conclusions: Our study demonstrates chrysin loaded PLGA-PEG promises a natural and efficient system for anticancer drug delivery to fight gastric cancer.

• 폴리머
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• 제34권3호
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• pp.253-260
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• 2010

본 연구에서는 조직확장 응용을 위한 생체적합성 생분해성 하이드로젤을 제조하고, 그 기본특성을 분석하였다. 친수성 고분자인 poly(ethylene glycol)의 양 말단에 다양한 몰비의 D,L-lactide와 glycolide를 개환 중합시켜 PLGA-PEG-PLGA 삼중공중합체를 합성한 뒤 비닐기를 도입하여 하이드로젤 제조 시 swelling/degradation controllers(SDC)로 사용하였다. 합성한 SDC와 PEG diacrylate를 사용하여 라디칼 중합으로 제조한 하이드로젤은 건조된 상태에서도 유연하고 탄성을 보였으며 분해테스트에서는 SDC의 조성과 SDC/PEG의 몰비에 따라 다양한 팽윤지연시간과 분해기간을 갖는 것으로 나타났다. 그 밖에 기계적 물성과 팽윤압력을 측정하였고, 이식시험을 통해 이식용 하이드로젤을 사용목적에 맞게 이식하거나 삽입하였을 때의 생체 조직의 국소적인 병리적 양상을 육안관찰과 현미경적 관찰을 통하여 평가하였다.

• Biomolecules & Therapeutics
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• 제16권4호
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• pp.425-430
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• 2008

The objectives of this study were to prepare PLGA film onto the surface of the capsular tension ring (CTR) for controlled drug release and investigate the influence of plasticizers, the test drug and measurement conditions on flexibility of the film. Film solutions were prepared by dissolving PLGA, plasticizer (triethyl citrate, TEC or polyethylene glycol, PEG), test drug (dexamethasone) in ethyl acetate then films were prepared by spray coating and evaporation method. Then, the flexibility of PLGA film was determined by elongation test. The addition of plasticizer, PEG or TEC to PLGA copolymer caused a depression of glass transition temperature ($T_g$) and the elasticity of PLGA films increased. The addition of dexamethasone to the PLGA/TEC matrix decreased the flexibility of film. Dimensional factors of the PLGA films such as width and thickness were significantly influenced on flexibility of films and film length and elongation speed had no considerable influence on elongation of films. In this study, sufficiently flexible and stable PLGA films capable of being coated onto CTR could be prepared. This PLGA films can be used as a platform for local drug delivery.

• Asian Pacific Journal of Cancer Prevention
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• 제17권5호
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• pp.2453-2457
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• 2016

Background: Dysregulation of HSP90 gene expression is known to take place in breast cancer. Here we used D,L-lactic-co-glycolic acid-polyethylene glycol-17-dimethylaminoethylamino-17-demethoxy geldanamycin (PLGA-PEG-17DMAG) complexes and free 17-DMAG to inhibit the expression of HSP90 gene in the T47D breast cancer cell line. The purpose was to determine whether nanoencapsulating 17DMAG improves the anti-cancer effects as compared to free 17DMAG. Materials and Methods: The T47D breast cancer cell line was grown in RPMI 1640 supplemented with 10% FBS. Encapsulation of 17DMAG was conducted through a double emulsion method and properties of copolymers were characterized by Fourier transform infrared spectroscopy and H nuclear magnetic resonance spectroscopy. Assessment of drug cytotoxicity was by MTT assay. After treatment of T47D cells with a given amount of drug, RNA was extracted and cDNA was synthesized. In order to assess HSP90 gene expression, real-time PCR was performed. Results: Taking into account drug load, IC50 was significant decreased in nanocapsulated 17DMAG in comparison with free 17DMAG. This finding was associated with decrease of HSP90 gene expression. Conclusions: PLGA-PEG-17DMAG complexes can be more effective than free 17DMAG in down-regulating of HSP90 expression, at the saesm time exerting more potent cytotoxic effects. Therefore, PLGA-PEG could be a superior carrier for this type of hydrophobic agent.

• Asian Pacific Journal of Cancer Prevention
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• 제16권9호
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• pp.3753-3758
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• 2015

Background: Polymeric nanoparticles are attractive materials that have been widely used in medicine for drug delivery, with therapeutic applications. In our study, polymeric nanoparticles and the anticancer drug, chrysin, were encapsulated into poly (D, L-lactic-co-glycolic acid) poly (ethylene glycol) (PLGA-PEG) nanoparticles for local treatment. Materials and Methods: PLGA: PEG triblock copolymers were synthesized by ring-opening polymerization of D, L-lactide and glycolide as an initiator. The bulk properties of these copolymers were characterized using 1H nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy. In addition, the resulting particles were characterized by scanning electron microscopy. Results: The chrysin encapsulation efficiency achieved for polymeric nanoparticles was 70% control of release kinetics. The cytotoxicity of different concentration of pure chrysin and chrysin loaded in PLGA-PEG ($5-640{\mu}M$) on T47-D breast cancer cell line was analyzed by MTT-assay. Conclusions: There is potential for use of these nanoparticles for biomedical applications. Future work should include in vivo investigation of the targeting capability and effectiveness of these nanoparticles in the treatment of breast cancer.

• KSBB Journal
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• 제17권1호
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• pp.33-37
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• 2002

PLGA 미립구로부터 G-CSF의 방출 거동 양상을 향상 시키기 위하여 G-CSF를 분자량 5000인 methoxy polyethylene glycol-aldehyde로 PEGylation 시켰다. 대부분의 G-CSF는 mono-PEGylation 되었으며, 이를 SDS-PAGE, HPLC, 및 펩타이드 지도 분석을 통해 확인하였다. W/O/W 방법을 사용하여 G-CSF 및 PEGylated G-CSF의 PLGA 미립구를 제조하였으며, 이때 봉입율은 높은 상태였다. 미립구내로 더 많은 G-CSF를 봉입하기 위하여 액상의 G-CSF 및 PEGylated G-CSF을 농축하였고 native gel과 gel filtration 크로마토 그래피를 통하여 단백질이 안정함을 확인하였다. 이렇게 제조한 PLGA 봉입체의 in vitro 방출 거동을 조사한 결과 PEGylated G-CSF는 native G-CSF에 비하여 더 오랜 시간 동안 방출이 지속되었고 최대 방출량도 증가하였다.

• 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.

• Asian Pacific Journal of Cancer Prevention
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• 제15권20호
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• pp.8693-8698
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• 2014

Background: Up-regulation of hsp90 gene expression occurs in numerous cancers such as lung cancer. D,L-lactic-co-glycolic acid-poly ethylene glycol-17-dimethylaminoethylamino-17-demethoxy geldanamycin (PLGA-PEG-17DMAG) complexes and free 17-DMAG may inhibit the expression. The purpose of this study was to examine whether nanocapsulating 17DMAG improves the anti cancer effect over free 17DMAG in the A549 lung cancer cell line. Materials and Methods: Cells were grown in RPMI 1640 supplemented with 10% FBS. Capsulation of 17DMAG is conducted through double emulsion, then the amount of loaded drug was calculated. Other properties of this copolymer were characterized by Fourier transform infrared spectroscopy and H nuclear magnetic resonance spectroscopy. Assessment of drug cytotoxicity on the grown of lung cancer cell line was carried out through MTT assay. After treatment, RNA was extracted and cDNA was synthesized. In order to assess the amount of hsp90 gene expression, real-time PCR was performed. Results: In regard to the amount of the drug load, IC50 was significant decreased in nanocapsulated(NC) 17DMAG in comparison with free 17DMAG. This was confirmed through decrease of HSP90 gene expression by real-time PCR. Conclusions: The results demonstrated that PLGA-PEG-17DMAG complexes can be more effective than free 17DMAG in down-regulating of hsp90 expression by enhancing uptake by cells. Therefore, PLGA-PEG could be a superior carrier for this kind of hydrophobic agent.