• Macromolecular Research
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• 제17권2호
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• pp.99-103
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• 2009

We evaluated the efficacy of pH-sensitive micelles, formed by methoxy poly(ethylene glycol)-b-poly($\beta$)-amino ester) (PEG-PAE), as carriers for paclitaxel (PIX), a drug currently used to treat various cancers. PTX was successful encapsulated by a film hydration method. Micelles encapsulated more than 70% of the PTX and the size of the PTX-encapsulated micelles (PTX-PM) was less than 150 nm. In vitro experiments indicated that the micelles were unstable below pH 6.5. After encapsulation of PTX within the micelles, dynamic light scattering (DLS) studies indicated that low pH had a similar demicellization effect. An in vitro release study indicated that PTX was slowly released at pH 7.4 (normal body conditions) but rapidly released under weakly acidic conditions (pH 6.0). We demonstrated the safety of micelles from in vitro cytotoxicity tests on HeLa cells and the in vivo anti-tumor activity of PTX-PM in B16F 10 tumor-bearing mice. We concluded that these pH-sensitive micelles have potential as carriers for anti-cancer drugs.

• 한국자기학회지
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• 제16권1호
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• pp.107-110
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• 2006

Emulsification-diffusion법에 의해 magnetite를 생분해성 고분자인 PLCA로 캡슐화 시켜 magnetite/PLGA 복합분말을 제조하였다. 이때 유기용매의 종류 변화가 얻어진 복합분말의 크기에 미치는 영향을 살펴보기 위해 다양한 종류의 유기용매[ethyl acetate(EA), propylene carbonate(PC), acetone (ACE)]가 사용되었으며, 분말의 입도분포는 동적 광산란법에 의해 측정되었다. 물에 부분적으로 용해되는 용매인 EA나 PC가 사용되었을 경우에는 80nm이하의 작은 크기의 복합분말이 얻어진 반면, 물에 잘 용해되는 용매인 ACE가 사용되었을 경우에는 330nm 이상의 큰 복합분말이 얻어졌다.

• 한국자기학회지
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• 제16권3호
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• pp.163-167
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• 2006

초음파 조사 및 계면활성제 첨가에 따른 입자의 변화를 연구하기 위하여 침전법, 음향화학적 침전법 그리고 게면활성제를 첨가한 음향화학적 침전법으로 나노 입자를 합성하였고, X-선 회절실험을 통하여 마그네타이트가 합성된 것을 확인하였다. 침전법, 음향화학적 침전법으로 합성한 입자의 크기는 계면활성제를 첨가한 음향화학적 침전법으로 합성한 입자보다 크게 얻어졌고, 초음파 출력이 증가 할수록 크기는 증가하였다. 계면활성제로 올레인 산을 첨가한 음향화학적 기법에서는 게면활성제의 농도에 따라 입자 크기를 선택적으로 조절하여 합성할 수 있었고, 단순 침전법이나 음향화학적 기법에서 보다 생성되는 입자의 크기 분포가 좁게 나타났다. 마그네타이트 나노 입자들의 자기적 특성을 SQUID를 통하여 분석한 결과, 실온에서 모두 초상자성 거동을 보이는 것으로 나타났다.

• Journal of Microbiology and Biotechnology
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• 제16권9호
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• pp.1369-1376
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• 2006

Self-organized nanogels were prepared from pullulan/biotin conjugates (PU/Bio) for the development of an effective anticancer drug delivery system. The degree of biotin substitution was 11, 19, and 24 biotin groups per 100 anhydroglucose units of pullulan. The physicochemical properties of the nanogels (PU/Bio1, 2 and 3) in aqueous media were characterized by dynamic light scattering, transmission electron microscopy, and fluorescence spectroscopy. The mean diameter of all the samples was less than 300 nm with a unimodal size distribution. The critical aggregation concentrations (CACs) of the nanoparticles in distilled water were $2.8{\times}10^{-2},\;1.6{\times}10^{-2}$, and $0.7{\times}10^{-2}mg/ml$ for the PU/Bio1, 2, and 3, respectively. The aggregation behavior of the nanogels indicated that biotin can perform as a hydrophobic moiety. To observe the specific interaction with a hepatic carcinoma cell line (HepG2), the conjugates were labeled with rhodamine B isothiocyanate (RITC) and their intensities measured using a fluorescence microplate reader. The HepG2 cells treated with the fluorescence-labeled PU/Bio nanoparticles were strongly luminated compared with the control (pullulan). Confocal laser microscopy also confirmed internalization of the PU/Bio nanogels into the cancer cells. Such results demonstrated that the biotin in the conjugate acted as both a hydrophobic moiety for self-assembly and a tumor-targeting moiety for specific interaction with tumor cells. Consequently, PU/Bio nanogels would appear to be a useful drug carrier for the treatment of liver cancer.

• Journal of Pharmaceutical Investigation
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• 제37권1호
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• pp.15-22
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• 2007

An oil-in-water solvent evaporation method was used to prepare the cyclosporin A (CyA)-loaded nanoparticles varying in poly (D,L-lactide-co-glycolide) (PLGA) polymer (RG 502H, RG 503H) and the amount of additive ethyl myristate (EM) or chitosan (CS). The particles were characterized for drug loading and entrapment efficiency by HPLC, surface morphology by scanning electron microscopy, particle size by dynamic light scattering and surface charge by Zetapotential. The results showed drug loadings ranging from 10.9% to 15.8% with high encapsulation efficiency (82.0-97.8%). SEM and DLS studies showed discrete and spherical particles with smooth surfaces and mean size ranging 257.6-721.7 nm. The additive EM or CS did not change the mean sizes of the nanoparticles, whereas by the coating effect of CS, the Zetapotential values of the CS-added nanoparticles were moved to the more positive direction as the amount of CS was increased. From the pharmacokinetic analysis, the nanoparticles formulations showed the higher bioavailability and MRT than $Neoral^{\circledR}$ While little adding effect of EM or CS was detected in pharmacokinetic profile when RG 503H was used as polymer carrier, more noticeable different pharmacokinetic behaviors could be observed in case of RC 502H. EM incorporation was found to elevate the $K_{el}$, whereas CS coating resulted in the decrease of F and $K_{el}$, which seems to be due to the function of CS as a barrier and a mucoadhesive coating.

• Journal of Pharmaceutical Investigation
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• 제40권6호
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• pp.353-356
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• 2010

Although liposomes have been applied as drug delivery systems in various fields, the usage was limited due to the low encapsulation efficiency compared to other carrier systems. Here, cationic liposomes were prepared by mixing 1,2-dioleoyl-3-trimethylammoniopropane (DOTAP) as a cationic lipid, 1,2-dioleoyl-sn-glycerol-phosphoethanolamine (DOPE) and cholesterol (CH), and the liposomes were hydrated by varying the aqueous phases such as phosphate-buffered saline (PBS), 5% dextrose, and 10% sucrose in order to improve the encapsulation efficiency of bovine serum albumin (BSA). The particle size and zeta potential were determined by dynamic light scattering method and in vitro release patterns were investigated by spectrophotometry. Particle size and zeta potential of liposomes were varied depending on the ratio of DOTAP/DOPE/CH in range of 270-350 nm and 0.8-9.7 mV, respectively. Moreover, the addition of polyethylene glycol (PEG) improved the encapsulation efficiency from 37% to 43% as well as reduced particle sizes of liposomes while the liposomes were hydrated in PBS. When the liposomes were hydrated with 10% sucrose, the encapsulation efficiency of BSA was higher than any other groups. Whereas PBS was used as hydration solution, lower encapsulation efficiency was obtained compared with other groups. More than 60% of BSA was released from the liposomes hydrated with 10% sucrose; thereafter another 20% of BSA was released. Therefore, release pattern of BSA from cationic liposomes was extended release in this study. From the results, cationic liposomes dispersed in 10% sucrose would be potential carrier with high encapsulation efficiency.

• 한국응용과학기술학회지
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• 제27권4호
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• pp.391-398
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• 2010

Soybean lecithin liposomes composed phosphatidyl choline, phosphatidyl ethanolamine, phosphatidyl inositol and phosphatidic acid were prepared by using the previously developed supercritical reverse phase evaporation method. The effect of phospholipid composition on the formation of liposomes and physicochemical properties were examined by means of trapping efficiency measurements, transmission electron microscopy, dynamic light scattering and zeta potential measurements. The trapping efficiency of liposomes for D-(+)-glucose made of CNA-Ⅰ which contains approximately 95% phosphatidyl choline is higher than that of CNA-II and CNA-O which contain approximately 32% phosphatidyl choline. However there is no any difference between the trapping efficiency of liposomes for D-(+)-glucose made of CNA-II which has saturated hydrocarbons tails and that of liposomes made of CNA-O which has unsaturated hydrocarbon chains. The electron micrographs of liposomes made of CNA-II and CNA-O show small spherical liposomes with diameter of $0.1\sim0.25{\mu}m$, while that of CNA-I shows large unilamellar liposomes with diameter of $0.2\sim1.2{\mu}m$. These results clearly show that phospholipid structure of phosphatidylcholine allows an efficient preparation of large unilamellar liposomes and a high trapping efficiency for water soluble substances. Liposomes made of CNA-II and CNA-O remained well-dispersed for at least 14 days, while liposome suspension made of CNA-I separated in two phase at 14 days due to aggregation and fusion of liposomes. The dispersibility of liposomes made of CNA-I is lower than that of CNA-II and CNA-O due to the smallar zeta potential of CNA-I.

• Bulletin of the Korean Chemical Society
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• 제33권11호
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• pp.3676-3680
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• 2012

An Epstein-Barr virus (EBV)-based plasmid contains the EBV nuclear antigen 1 (EBNA1) gene and EBV replication origin (oriP) sequence. Since EBNA1 (the only EBV-encoded protein) is combined with oriP, it is replicated simultaneously with chromosomal DNA in human, primate, and canine cells and is faithfully segregated at a stable copy number upon cell division. Consequently, it can be used to stably express gene inserts over a prolonged time in target cells. We have previously shown that the polyamidoamine (PAMAM) dendrimer can be surface-modified with L-arginine. Arginine is present at a high frequency in the transactivator of transcription (Tat) sequences of human immunodeficiency virus (HIV). It presents high membrane permeability and permits effective transfer of DNA inside the cells. In this study, we constructed two kinds of recombinant DNA by inserting the luciferase gene and enhanced green fluorescence protein (eGFP) gene as reporter genes into the pCEP4 plasmid vector. We measured dynamic light scattering (DLS) and zeta potential after preparing PAMAM-based cationic polymer/EBV-based plasmid complexes. We performed transfection of HEK 293 cell lines with the polyplexes, and monitored luciferase activity and green fluorescence protein (GFP) expression. Our results show that PAMAM-based cationic polymer/EBV plasmid complexes provide enhanced and sustained gene expression.

• Korean Chemical Engineering Research
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• 제50권2호
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• pp.191-197
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• 2012

Isophorone diisocyanate(IPDI), polycarbonate diol(PCD), dimethylol propionic acid(DMPA)를 출발물질로 하여 제조된 폴리우레탄 prepolymer의 미반응 NCO기를 아크릴 단량체인 pentaerythritol triacrylate(PETA)로 capping시켜 acrylic terminated polyurethane prepolymer를 합성하였다. 그 후 이 prepolymer의 잔여 NCO기를 실란커플링제인 aminopropyl triethoxysilane(APS) 또는 glycidoxypropyl trimethoxysilane(GPTMS)와 반응시켜 silylated acrylic terminated waterborne polyurethane을 제조하였다. 동적 빛 산란법에 의해 측정된 순수한 수분산 폴리우레탄의 평균 직경은 PETA와 APS가 첨가됨에 따라 14.3 nm에서 208.6 nm로 크게 증가하였다. 또한 silylated acrylic terminated waterborne polyurethane 코팅 도막의 연필경도 및 내마모성은 순수한 수분산 폴리우레탄보다 우수하였다.

• Bulletin of the Korean Chemical Society
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• 제34권2호
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• pp.558-564
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• 2013

A simple and effective method is introduced to synthesize a series of polystyrene-b-poly(oligo(ethylene oxide) monomethyl ether methacrylate)-b-polystyrene (PSt-b-POEOMA-b-PSt) triblock copolymers. The structures of PSt-b-POEOMA-b-PSt copolymers were characterized by Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance ($^1H$ NMR) spectroscopy. The molecular weight and molecular weight distribution of the copolymer were measured by gel permeation chromatography (GPC). Furthermore, the self-assembling and drug-loaded behaviours of three different ratios of PSt-b-POEOMA-b-PSt were studied. These copolymers could readily self-assemble into micelles in aqueous solution. The vitamin E-loaded copolymer micelles were produced by the dialysis method. The micelle size and core-shell structure of the block copolymer micelles and the drug-loaded micelles were confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The thermal properties of the copolymer micelles before and after drug-loaded were investigated by different scanning calorimetry (DSC). The results show that the micelle size is slightly increased with increasing the content of hydrophobic segments and the micelles are still core-shell spherical structures after drug-loaded. Moreover, the glass transition temperature (Tg) of polystyrene is reduced after the drug loaded. The drug loading content (DLC) of the copolymer micelles is 70%-80% by ultraviolet (UV) photolithography analysis. These properties indicate the micelles self-assembled from PSt-b-POEOMA-b-PSt copolymers would have potential as carriers for the encapsulation of hydrophobic drugs.