• 생명과학회지
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• 제12권6호
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• pp.745-751
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• 2002

원유 분해능이 강력한 해양균주를 얻고자 유류오염 지역으로부터 crude oil을 탄소원으로 이용하는 수십 종을 분리하였다. 분리된 균주중 원유분해능 및 biosurfactant 생성능이 우수한 균주를 선별하여, 형태학적, 생화학적 및 생리학적 특성을 조사한 후 Bacizzus sp. LSC11로 동정하였다. Bacillus sp. LSC11 균주 배양액의 표면장력은 최저 32mN/m까지 감소되었다. Biosurfactant의 CMC값은 0.0035% (w/v) 인 것으로 나타났다. Bacillus sp. LSC11가 생산하는 biosurfactant의 유화활성은 대두유에서 최대였으며, 원유에서도 높은 편이였다. 유화안정성은 합성계면활성제와 비슷하거나 우수하였다.

• Journal of Pharmaceutical Investigation
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• 제36권3호
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• pp.175-184
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• 2006

Poly(D,L-lacic acid)(PLA) microshperes containing loazepam were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of lorazepam to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like lorazepam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of lorazepam for long-acting injectable delivery system in vitro, which would aid in Predicting in vivo release Profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

• Archives of Pharmacal Research
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• 제28권9호
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• pp.1092-1096
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• 2005

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

• Journal of Pharmaceutical Investigation
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• 제41권3호
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• pp.185-190
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• 2011

The purpose of this study was to evaluate the phagocytic uptake of surface modified PLGA microspheres containing ovalbumin (OVA) into dendritic cell. In order to find the most suitable formulation for targeted delivery to antigen presenting cells (APC), OVA was encapsulated by a double emulsion solvent evaporation method with three PLGA microspheres (PLGA 50:50, PLGA 75:25 and PLGA 85:15) and two surface modified microspheres by chitosan and sodium dodecyl sulfate (SDS). Physicochemical properties were evaluated in terms of size, zeta potential, encapsulation efficiency, different scanning calorimeter (DSC), x-ray diffraction, morphology, and OVA release test from microspheres. Phagocytic activity was estimated using dendritic cells and analyzed by fluorescence activated cell sorter (FACS). The result showed that zeta potential of PLGA particles was changed to positive by the chitosan modification. The release profile of chitosan modified PLGA microspheres exhibited sustained release after initial burst. The chitosan modified microspheres had higher phagocytic uptake than the other microspheres. Such physicochemical properties and phagocytic uptake studies lead us to conclude that chitosan modified microspheres is more suitable formulation for the targeted delivery of antigens to APC compared with the other microspheres.

• 약학회지
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• 제44권4호
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• pp.293-299
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• 2000

Biodegradable microspheres made from poly-lactide-co-glycolide polymers have been considered as a new delivery system for single-dose vaccine. Purified tetanus toxoid (TT) was encapsulated in poly-lactide(PLA) and poly-lactide-co-glycolide (PLGA) microparticles using a solvent evaporation method in a multiple emulsion system (water-in oil-in water). The morphology of 77-loaded microparticles was spherical and the suface of them was smooth. The particle size was in a range of 2-10. Protein loading efficiency was 68-97.8%. PLGA (85:15) microparticle showed the highest efficiency. Protein release pattern was influenced by polymer molecular weight and composition. The release rate of PLA(Mw 100,000) microsphere was higher than any other microspheres. In consequence of the hydrolysis of PLGA(50:50) microspheres, environmental pH decreased from 7.4 to 5.0. The PLA, PLGA (75:25) and PLGA (85:15) microshperes showed no significant pH change. The antigenicity or n in microshperes was assayed by indirect sandwich ELISA using equine polyclonal tetanus antitoxin for capture antibody and human polyclonal tetanus antitoxin for primary antibody. The antigenicity of TT in PLA (Mw 100,000), PLGA(50:50, Mw 100,000) and PLGA (75:25, Mw 73,300) after 30 days incubation showed 54, 40.9 and 76.7%, respectively.

• 폴리머
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• 제26권3호
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• pp.326-334
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• 2002

본 실험에서는 PCL 마이크로캡슐을 제조하여 형태적 분석 및 제조 조건에 따른 특성을 살펴보고 약물방출거동을 통하여 약물전달체계로서의 가능성을 고찰하였으며 액중건조법을 사용하여 약물을 함유한 마이크로캡슐을 제조하였다. 마이크로캡슐 입경과 형태는 교반속도, 교반시간 그리고 유화제의 농도에 따라 어떠한 영향을 받는가에 대하여 관찰하였다. 마이크로캡슐의 모양과 표면을 image analyzer와 SEM으로 관찰한 결과 제조된 마이크로캡슐은 평균 입경이 40~400$\pm$20 $mu extrm{m}$로 주름이 발달된 구형의 형태였다. 제조된 PCL 마이크로캡슐의 약물함유 여부는 FT-IR을 사용하여 확인하였고 접촉각 측정을 통해 PCL과 약물간의 계면에서의 부착일을 살펴보았다. 또한 방출거동을 살펴보기 위해 UV/vis. 흡광광도법으로 흡광도를 측정하여 용출된 약물비 양을 정량 하였으며, 그 결과, 유화제의 농도를 높게 하여 제조한 마이크로캡슐의 약물 방출이 상당히 빠름을 알 수 있었다.

• 폴리머
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• 제28권2호
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• pp.103-110
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• 2004

토코페롤을 함유하는 폴리($\varepsilon$-카프로락톤)(PCL) 마이크로캡슐은 액중건조법에 의하여 제조하였고, 제조 조건에 따른 마이크로캡슐의 특성과 PCL 필름을 사용하여 PCL의 분해거동을 측정하였다 제조된 마이크로캡슐의 크기 및 형태와 구조적 특성은 각각 SEM과 XRD를 이용하여 관찰하였다. 또한, 접촉각 측정을 통하여 심물질의 농도에 따른 마이크로캡슐의 표면자유에너지를 측정하였다. 실험결과, 마이크로캡슐은 유화제로 폴리(비닐 알코올)을 사용한 경우 안정된 구형의 마이크로캡슐이 형성되었고, 마이크로캡슐의 표면자유에너지와 PCL의 결정성은 감소하고, PCL 필름은 악 21일 후 분해가 시작되었다. 토코페롤의 방출특성은 UV/vis.에 의하여 측정하였으며, 마이크로캡슐의 방출속도는 교반속도의 증가와 함께 증가하였다. 이는 교반속도의 증가와 함께 감소된 마이크로캡슐 입자 크기에 의한 방출용액과 마이크로캡슐 사이의 계면의 증가에 의한 것으로 판단된다.

• KSBB Journal
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• 제19권3호
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• pp.178-186
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• 2004

복합한방 재료인 옥용산에 대해 UV 흡수능, tyrosinase 저해활성 그리고 free radical 소거활성을 측정함으로서 미백활성을 검정하고 비교 시험군으로서 비타민C와 함께 Eudragit 이 코팅된 coconut oil을 이용한 SLN을 제조할 수 있었다. 실험 결과, 옥용산은 UV 영역에서 흡수능을 가지며 tyrosinase 저해 활성과 free radical 소거활성을 가진 것으로 확인되었다. 제조된 E-SLN을 TEM을 이용하여 관찰한 결과 크기 50∼300 nm인 구형의 양호한 입자를 형성하고 있음을 확인하였다. 또한 그 크기분포와 캡슐화 효율 분석을 통해 EUD의 농도가 2.0% (w/v), w/o 비율은 1 ： 9, emulsion과 pour solution의 비율은 1 : 10, 그리고 실온에서 제조한 E-SLN의 캡슐화 효율이 가장 높고 크기의 분포가 가장 양호한 것을 알 수 있었다. E-SLN을 이용하여 in vitro 방출시험을 실시한 결과 E-SLN은 pH와 온도 의존적으로 약물을 방출하는 경향을 나타냈다. 결과적으로 제조된 E-SLN은 pH와 온도 의존적으로 약물을 전달할 필요가 있는 계에 대한 약물전달 시스템으로 적합할 것으로 보인다. 폐쇄 첩포시험과 자외선 조사에 의한 인공색소침착과 시료도포에 의한 미백효능 판정에 의한 임상시험 결과 옥용산과 비타민C, 그리고 이를 포함하는 E-SLN은 대조군의 경우와 비교하여 미백효과를 가지는 것으로 확인되었으며 이는 기능성화장품에의 응용 가능성을 높여주었다.

• Journal of Pharmaceutical Investigation
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• 제38권1호
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• pp.63-72
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• 2008

Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to $PLA^{\circ}{\AE}s$ with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.

• Journal of Pharmaceutical Investigation
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• 제40권2호
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• pp.85-90
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• 2010

Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.