• Title/Summary/Keyword: dry liposome

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Preparation and Evaluation of Aclarubicin Liposome using Microfluidizer (마이크로플루다이저를 이용한 아클라루비신 리포좀의 제조 및 평가)

  • Park, Mork-Soon;Park, Jin-Kyu;Lee, Gye-Won;Baek, Myoung-Ki;Jee, Ung-Kil
    • YAKHAK HOEJI
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    • v.42 no.3
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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.

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Effect of Dehydration and Rehydration of the pH-Sensitive Liposomes Containing Chimeric gag-V3 Virus Like Particle on Their Long-term Stability

  • Chang, Jin-Soo;Park, Myeong-Jun;Kim, Tae-Yeon;Woo, Gyu-Jin;Chung, Soo-il;Cheong, Hong-Seok
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.4 no.1
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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.

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Effects of Maltose on the Stability of Freeze-Dried Liposomes (동결 건조된 리포솜의 안정화에 있어서 말토스의 영향)

  • Kim, Yun-A;Han, Hee-Dong;Shin, Byung-Cheol
    • Journal of the Korean Chemical Society
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    • v.48 no.6
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    • pp.616-622
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    • 2004
  • Liposome powders were prepared by a freeze-drying method for the application to the field of drug carrier. The effect of maltose as a liposome stabilizer was studied on the stability and the drug-loading efficiency of the freeze-dried liposome powders. The particle size of liposomes before and after freeze-drying was determined to evaluate the liposome stability. The drug-loading efficiency was measured by Fluorescence spectrophotometer using calcein as a model drug. When maltose was added after the preparation of the liposomes, the liposomes was stable, compared to the case of maltose addition at the hydration procedure. By the addition of maltose, the liposome was stable for 30 days at $4{\sim}37^{\circ}C$, while the particle size of the liposome without maltose increased with time. The liposome showed relatively high stability when the maltose/lipids molar ratio was 3 and 6.

Characteristics and Drug Release Profiles of Multilamellar Vesicle(MLV) and Microemulsified Liposome(MEL) Entrapped 5-Fluorouracil and Its derivatives (5-Fluorouracil과 그 유도체를 봉입한 Multilamellar Vesicle(MLV)과 Microemulsified Liposome(MEL)의 특성 및 약물방출 거동)

  • Jee, Ung-Kil;Park, Mok-Soon;Lee, Gye-Won;Lyu, Yeon-Geun
    • Journal of Pharmaceutical Investigation
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    • v.25 no.3
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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).

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Evaluation of Physical Properties of Liposome Essences as Customized Cosmetic Bases and Evaluation of Satisfaction According to Skin Type (맞춤형화장품 베이스로서 리포좀 에센스의 물성 평가 및 피부타입에 따른 만족도 평가)

  • An, Hyung Guen;Hyeon, Tong-Il;Yoon, Kyung-Sup
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.48 no.1
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    • pp.1-10
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    • 2022
  • Customized cosmetics are continuously mentioned as a trend in the cosmetics industry to respond to the recent rapid changes in the social environment and pursue individuality and diversity. Accordingly, four types of liposome essence corresponding to skin types were prepared by varying the ratio of liposome formulation and essence formulation as a customized cosmetic base that can be easily mixed and applied at the workplace. The volatilization residues of four types of liposome essence were measured and the nanoparticle size, polydispersity index, zeta potential and viscosity according to time for 90 d were measured, and Turbiscan was measured as a method for evaluating the stability of a colloidal dispersion system. In addition, a simple usability evaluation was performed for four types of liposome essence corresponding to the skin type. As a result, the amount of volatile residue in the four types of liposome essence was increased in dry products rather than oily ones, and the particle size showed a tendency to increase with time in the range of 165 to 175 nm, increasing up to 31.5%, and the polydispersity index was 0.23 to 0.26. There was little change with time, and the zeta potential was -74 to -72 mV, showing a slight decrease with time, but there was little change to the extent of a maximum decrease of 14.0%. Viscosity showed a decreasing trend with time in the range of 2,580 ~ 3,290 cps, showing a maximum decrease of 17.5%. In the turbiscan measurement, all of the turbiscan stability index, a measure of stability, were less than 1.0, indicating dispersion stability. In the overall simple usability satisfaction evaluation for skin types (6 points), products for oily skin (5.33 ± 0.75 points) > products for medium dry skin (5.13 ± 0.95 points) > products for dry skin (5.03 ± 0.96 points) > products for oily skin (4.80 ± 1.04 points) points) were evaluated in order. The four types of liposome essence corresponding to skin types with different ratios of liposome formulation and essence formulation were physically stable, and the possibility of application as a customized cosmetic base according to skin type was confirmed.

The effect of liposomal cephalexin on the dry period treatment of bovine Staphylococcus aureus mastitis (젖소의 Staphylococcus aureus성 유방염에 대한 liposomal cephalexin 의 건유기 치료효과)

  • Shin, Jin-ho;Han, Hong-ryul
    • Korean Journal of Veterinary Research
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    • v.32 no.2
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    • pp.251-258
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    • 1992
  • Liposomal cephalexin was used m the dry period treatment of bovine mastitis due to Staphylococcus aureus. Liposomes were prepared by stable plurilamellar vesicle(SPLV) process. The shape and size of SPLVs were examined by transmission electron microscopy. The entrapping efficiency and stability of SPLVs were determined by high performance liquid chromatography or liquid scintillation counting. The size of SPLVs ranged from 0.1 to $4.01{\mu}m$ in diameter, with an entrapping efficiency of cephalexin of 25.8 %. The formulation of liposomal cephalexin was used for treatment were SPLV-entrapped cephalexin and free cephalexin with total cephalexin concentration of 250mg per quarters. All quarters were infused intramammarily at the end of lactation period by liposomal cephalexin, free cephalexin, or blank liposome with free cephalexin. The number of quarters cured by liposomal cephalexin(14/15 quarters, 93 %) was significantly higher than that by free cephalexin(7/15 quarters, 46%). or by blank liposome with free cephalexin(8/15 quarters, 53 % ) (p<0.05).

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Characterization and Evaluation of Freeze-dried Liposomes Loaded with Ascorbyl Palmitate Enabling Anti-aging Therapy of the Skin

  • Lee, Sang-Kil;Lee, Jae-Hwi;Choi, Young-Wook
    • Bulletin of the Korean Chemical Society
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    • v.28 no.1
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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.

Preparation and Evaluation of Proliposome (프로리포솜의 제조 및 평가)

  • Chung, Dae-Sik;Shim, Chang-Koo;Lee, Min-Hwa;Kim, Shin-Keun
    • YAKHAK HOEJI
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    • v.32 no.4
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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.

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Considerations for Making Liposomes by Thin Film-Hydration Method

  • Gyeong-Tak Byeon;Ji-Yoon Son;Jeongsoo Yoo
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.8 no.2
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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.

Various Types and Manufacturing Techniques of Nano and Micro Capsules for Nanofood

  • Kim, Dong-Myong
    • Journal of Dairy Science and Biotechnology
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    • v.24 no.1
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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.

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