• 약학회지
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• 제42권3호
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• pp.265-274
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• 1998

In order to attain a sustained release at targeted organs in a prolonged time which can reduce the side effects and maximize the therapeutic effect, aclarubicin (ACL) was entrap ped into liposomes of different lipid compositions using Microfluidizer, and dry liposomes were prepared by lyophilization. The dry aclarubicin-entrapped liposomes were evaluated in terms of mean particle size and size distribution, entrapment efficiency and in vitro drug release profile. The Entrapment efficiency of liposome, when the concentration of aclarubicin and lipid were 0.5 to 1.0mg/ml and $200{\mu}mol$/ml, respectively, was over 80% using Microfluidizer, in contrast to 70% of entrapment efficiency using hand-shaking method. Mean particle size and size distribution of aclarubicin-entrapped liposomes of various lipid compositions did not change considerably by the freeze drying. The range of particle size was between 80 and 200nm. Among aclarubicin-entrapped liposomes, ACL-liposome of PC/DPPC/CH0L/TA displayed the most significant sustained release. The addition of DPPC appeared to be favorable for the control of release. In general, aclarubicin entrapped in liposomes was less stable than free aclarubicin either in pH 7.4 phosphate buffer or in human plasma. Formulation I($t_{1/2}$, 20.3 hr) devoid of lipid additive was the most unstable in the phosphate-buffer solution while formulation II($t_{1/2}$, 40.7 hr) with cardiolipin was the most stable. Half lives of aclarubicin-entrapped liposomes in human plasma were 43.2, 50.7, 35.9 and 35.3 hr for formulation I. II, III and IV, respectively, in contrast to 57.8 hr for free aclarubicin.

• Biotechnology and Bioprocess Engineering:BBE
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• 제4권1호
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• pp.66-71
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• 1999

One of the practical limitations with the use of liposomes for delivery of the pharmaceutical substances such antigens is that liposomes are relatively unstable in storage. In order to extend the stability of liposome in storage without affecting their functional activity, solution-type liposomes were dehydrated to form a structurally intact dry liposomes. Comparative immunological evaluation was carried out for both dry and solution-type liposomes containing gag-V3 chimera, consequently it was found that dry liposomes elicited both humoral and cellular response as efficiently as solution-type liposemes did against the same gag-V3 antigen. Especially, long-term stability of the liposomes was remarkably enhanced by the dehydration made to loposomes without a significant change in its ability to elicit immune response in vivo. These results indicate that dry pH-sensitive liposome may become an effective delivery and adjuvant system for general vaccine development.

• 대한화학회지
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• 제48권6호
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• pp.616-622
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• 2004

약물 수송체로 사용되는 리포솜은 동결 건조를 통하여 분말화 시키는 방법이 사용되어지고 있다. 리포솜 안정제로서 말토스는 동결건조된 리포솜 분말의 안정성을 향상시키고 약물 봉입률에 영향을 주는 것으로 알려져 왔다. 동결건조 전과 후의 리포솜 입자의 크기를 측정하므로서 리포솜의 안정성을 평가하였고 또한, 약물 봉입률은 모델 약물인 칼세인을 사용하여 조건에 따른 봉입양을 측정하였다. 리포솜 제조 후에 말토스를 첨가한 리포솜은 수화하는 과정에서 말토스를 첨가하여 제조한 리포솜보다 훨씬 더 안정한 것으로 확인되었다. 말토스를 첨가하지 않은 리포솜은 시간이 지남에 따라 입자의 크기가 커지는 반면, 리포솜 제조 후에 말토스를 첨가한 리포솜은 $4{\sim}37^{\circ}C$에서 30일 동안 안정하다. 또한, 말토스/지질의 물농도 비가 3과 6일 때 상대적으로 가장 높은 안정성을 보였다.

• Journal of Pharmaceutical Investigation
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• 제25권3호
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• pp.249-264
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• 1995

Although liposome has many advantages as a pharmaceutical dosage form, its application in the industrial field has been limited because of some problems such as preparation method, reproducibility, scale-up, stability and sterilization etc. Liposomes prepared by microemulsification method had defined size, narrow size distribution, reproducibility and high entrapment efficiency. For enhancing the stability, the dry form of liposome was recommended. These types of liposome are proliposome and freeze-dried liposome. The liposome must have some properties for preparing of freeze-dried liposome; small size $(50{\sim}200\;nm)$, narrow size distribution and cryoprotectant. In this experiment, the liposomes containing 5-Fluorouracil(5-FU) and its prodrug(pentyl-5-FU-1-acetate; PFA, hexyl-5-FU-1-acetate; HFA) were made with soybean phosphatidylcholine, cholesterol, stearylamine(SA) and dicetyl phosphate(DCP) employing hydration method or microemulsification method using $Microfluidizer^{TM}$. Both or liposome types were MLV and MEL. After preparation, freeze drying and rehydration were performed. In the process of freezing, trehalose(Tr) was added as a cryoprotectant. Their evaluation methods were as follows; entrapment efficiency, mean particle size and size distribution, dissolution test, retain of entrapment efficiency and turbidity after freeze-drying. The results are summarized as belows. The entrapment efficiency of 5-FU was dependent on total lipid concentration and cholesterol content but that of PFA and HFA was decreased when cholesterol was added. When DCP and SA were added, entrapment efficiency was decreased. As the partition coefficient of drug was increased, entrapment efficiency was increased. Under the same condition, entrapment efficiency of MEL is similar to that of MLV. The mean particle size and size distribution of MEL were smaller than those of MLV. Dissolution rates of drug from both liposome types were comparatively similar. Dissolution rates of drugs with serum and liver homogenate were faster than without these material. After preparation of liposome, free drug was removed efficiency by Dowex 50W-X4. When liposome was freeze-dried and then rehydrated in the presence of Tr, characteristics of liposome were maintained well in MEL than MLV. Tr Was used successfully as a cryoprotectant in the process of freeze drying and the optimal ratio of Tr:Lipid was 4:1(g/g).

• 대한화장품학회지
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• 제48권1호
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• pp.1-10
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• 2022

맞춤형화장품은 화장품산업에서 최근 사회환경의 빠른 변화에 대한 대응, 개성과 다양성을 추구하는 트렌드로서 지속적으로 언급되고 있다. 이에 사업장에서 용이하게 혼합하여 적용할 수 있는 맞춤형화장품 베이스로 리포좀 제형과 에센스 제형의 비율을 달리함으로써 피부타입에 대응한 리포좀 에센스 4 종을 제조하였다. 리포좀 에센스 4 종에 대한 휘발잔분 측정과 90 일 동안의 시간에 따른 나노 입자크기, 다분산지수, 제타전위 및 점도를 측정하였으며, 콜로이드 분산계의 안정성 평가방법으로서 터비스캔을 측정하였다. 또한 피부타입에 대응한 리포좀 에센스 4 종에 대해 간이 사용성 평가를 진행하였다. 결과, 리포좀 에센스 4 종은 지성용보다는 건성용 제품에서 휘발잔분량이 증가하였으며, 입자크기는 165 ~ 175 nm 범위로 시간에 따라 증가 경향을 보여 최대 31.5%까지 증가하였고, 다분산지수는 0.23 ~ 0.26 정도로 시간에 따른 변화는 거의 없었으며, 제타전위는 -74 ~ -72 mV로 시간에 따라 약간 감소 경향을 보이나 최대 14.0% 감소하는 정도로 변화가 거의 없었다. 점도는 2,580 ~ 3,290 cps 범위로 시간에 따라 감소 경향을 보여 최대 17.5% 감소를 보였다. 터비스캔 측정에서는 안정성의 척도인 turbiscan stability index가 모두 1.0 이하로 분산 안정성을 보였다. 피부타입 대응 전체적인 간이 사용성 만족도 평가(6 점법)에서는 중지성 피부용 제품(5.33 ± 0.75 점) > 중건성 피부용 제품(5.13 ± 0.95 점) > 건성 피부용 제품(5.03 ± 0.96 점) > 지성 피부용 제품(4.80 ± 1.04 점) 순으로 평가되었다. 리포좀 제형과 에센스 제형의 비율을 달리한 피부타입 대응 리포좀 에센스 4 종은 물성적으로 안정하며, 피부타입에 따른 맞춤형화장품 베이스로서의 적용 가능성을 확인하였다.

• 대한수의학회지
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• 제32권2호
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• pp.251-258
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• 1992

Stable plurilamellar vesicle(SPLV) 제작법을 이용한 liposomal cephalexin으로 젖소의 Staphylococcus aureus성 유방염에 대해 건유기 치료를 시도하였다. SPLV의 모양과 크기를 transmission electron microscopy로 관찰하였으며 SPLV의 포획율 및 안정성은 high performance liquid chromatography 및 liquid scintillation counting으로 조사한 바 SPLV의 크기는 대개 직경 $0.1{\sim}4.0{\mu}m$였고, cephalexin 포획율은 $25.8{\pm}3.1$ $(mean{\pm}SE)$였으며 $4^{\circ}C$ 보관시 0, 24, 48, 72 및 96 시간후의 유리농도백분율은 각각 1.1, 3.9, 6.5, 7.5 및 8.4%였다. S aureus에 감염된 45분방에 대하여 15분방씩 3군으로 나누어 각 분방당 250mg의 liposomal cephalexin(LC군), 250mg free cephalexin(FC)군 및 blank liposome을 첨가한 250mg cephalexin(BLC)군을 건유시 분방내 주입한 후 분만당일에 균분리 및 동정을 실시한 바 LC군, FC군 및 BLC군에서 각각 1, 8 및 7분방에서 상기와 동일한 균이 분리되어 LC군이 타군에 비해 유의한 치료효과를 나타내었다.

• Bulletin of the Korean Chemical Society
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• 제28권1호
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• pp.99-102
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• 2007

To prepare freeze-dried ascorbyl palmitate (AsP)-containing liposome which can protect the drug from moisture attack and be used instantly by mixing with water for anti-aging and skin whitening therapy, AsP was encapsulated into liposomes and freeze-dried with trehalose. The freeze-dried liposome formulations were characterized by measuring water contents, particle size, time required for complete reconstitution. With the freeze-dried liposomes, we performed the stability test under accelerated conditions, skin permeation and localization test. The measurement of the time to perfect reconstitution showed that the freeze-dried liposomes can be changed to their initial state rapidly and short term stability test of AsP in reconstituted liposomes under accelerated conditions confirmed that the stability of AsP was considerably enhanced as compared to freshly prepared liposomes. The skin permeation and localization properties of AsP in reconstituted liposomes were not significantly different, indicating that the liposomal structures were maintained before and after freezedrying. In conclusion, the freeze-drying method provided a possible way to overcome the instability issue of AsP induced by the moisture and reproduced similar skin permeation and localization properties as shown by freshly prepared liposomes.

• 약학회지
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• 제32권4호
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• pp.234-238
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• 1988

Proliposome of Sudan IV was prepared according to Payne et al. and evaluated for it's size distribution, surface characteristics and conversion to liposome in aqueous medium. The manufacturing procedures for proliposomes involve the coating of phospholipid solution with Sudan IV on the surface of sorbitol particle in rotary vacuum evaporator. As a result, dry, free flowing and stable proliposome was obtained and multi-lamellar liposome of sudan IV was formed spontaneously when water were added to this. Proliposomes were expected as a probable answer for the physical instability of conventional liposomes.

• 대한방사성의약품학회지
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• 제8권2호
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• pp.151-156
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• 2022

Liposomes are bilayered particles that are surrounded by an aqueous solvent with amphiphilic substances such as phospholipids. Liposomes have the potential to overcome the limitations of physiochemical properties of existing drugs, and are therefore widely used in research for the treatment of many diseases, especially cancer. Currently, there are many liposome manufacturing methods that use various lipids and amphiphiles. Among them, the thin film-hydration method is a traditional and very simple method to prepare liposomes by hydrating a dry lipid film in an aqueous solvent, which has been widely used in the laboratory until recently. Recently, approaches to new nuclear imaging agents and radiotherapy by loading radioactive isotopes inside liposomes have been actively studied. In this review, we would like to discuss considerations for preparing liposomes using the thin film-hydration method.

• Journal of Dairy Science and Biotechnology
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• 제24권1호
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• pp.53-63
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• 2006

Nano and micro capsulation (NM capsulation) involve the incorporation for nanofood materials, enzymes, cells or other materials in small capsules. Since Kim D. M. (2001) showed that a new type of food called firstly the name of nanofood, which means nanotechnology for food, and the encapsulated materials can be protected from moisture, heat or other extreme conditions, thus enhancing their stability and maintaining viability applications for this nanofood technique have increased in the food. NM capsules for nanofood is also utilized to mask odours or tastes. Various techniques are employed to form the capsules, including spray drying, spray chilling or spray cooling, extrusion coating, fluidized bed coating, liposome entrapment, coacervation, inclusion complexation, centrifugal extrusion and rotational suspension separation. Each of these techniques is discussed in this review. A wide variety of nanofood is NM capsulated - flavouring agents, acids, bases, artificial sweeteners, colourants, preservatives, leavening agents, antioxidants, agents with undesirable flavours, odours and nutrients, among others. The use of NM capsulation for sweeteners such as aspartame and flavors in chewing gum is well known. Fats, starches, dextrins, alginates, protein and lipid materials can be employed as encapsulating materials. Various methods exist to release the ingredients from the capsules. Release can be site-specific, stage-specific or signaled by changes in pH, temperature, irradiation or osmotic shock. NM capsulation for the nanofood, the most common method is by solvent-activated release. The addition of water to dry beverages or cake mixes is an example. Liposomes have been applied in cheese-making, and its use in the preparation of nanofood emulsions such as spreads, margarine and mayonnaise is a developing area. Most recent developments include the NM capsulation for nanofood in the areas of controlled release, carrier materials, preparation methods and sweetener immobilization. New markets are being developed and current research is underway to reduce the high production costs and lack of food-grade materials.