• Title/Summary/Keyword: 리포솜

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Surface Modification of Liposomes Using Comblike Copolymer for Enhancing Stability in Blood Circulation (혈류 내 안정성 향상을 위한 빗 모양 고분자로 개질된 리포솜)

  • Sin, Byeong-Cheol;Song, Chung-Gil;Hwang, Tae-Won;Seong, Ha-Su;Park, Eun-Seok
    • Journal of the Korean Chemical Society
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    • v.50 no.3
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    • pp.216-223
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    • 2006
  • To increase the stability of liposomes in blood circulation, surface modification of liposomes by incorporating a lipid-polymer derivative in the lipid bilayer or conjugating a hydrophilic polymer to the liposomal surface has been developed. In this study, the comblike copolymer, poly(HEMA-co-HPOEM), having multiple polyethyleneoxide side chains was prepared by free radical polymerization of hydroxyethylmethacrylate (HEMA) and hydroxypolyoxyethylenemethacrylate (HPOEM) as vinyl monomers. Poly(HEMA-co-HPOEM) was conjugated to the liposomal surface and the characteristics of the modified liposomes in serum were investigated. Conjugation of poly(HEMA-co-HPOEM) to liposomes increased the particle size of the liposomes by 30 nm and decreased the absolute value of zeta potential of the liposomes by shielding the negative charge of liposomal surface. Loading efficiency of model drug, doxorubicin, in liposomes was about 90% and the efficiency was not affected by conjugation of poly(HEMA-co-HPOEM) to liposomes. The particle size of poly(HEMA-co-HPOEM)-conjugated liposomes in serum did not changed and the protein adsorption was lower than that of control liposomes or liposomes containing polyethyleneoxide-lipid derivative (PEG-liposomes). These results suggest that poly(HEMA-co-HPOEM) is efficient for the stabilization of liposomes in blood circulation.

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.

Preparation and Stability Measurement of Liposome-amino Acid Conjugates (리포솜-아미노산 결합체의 제조와 안정성 측정)

  • 문제영;이기영;김진철
    • KSBB Journal
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    • v.15 no.1
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    • pp.96-99
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    • 2000
  • Liposome-amino acid conjugates were prepared using phopholipid (dipalmitoylphosphatidylcholine (DPPC) or distearoylph-osphatidylcholine(DSPC)) and hydrophobically modified amino acids (glutamic acid(glu), glutamine(gln) or asparagine(asn)). The size of liposomes was about 100 nm. According to the glucose-induced turbidity changes, liposomes composed of DPPC and glutamic acid have higher glucose binding affinity than liposomes of DPPC-glutamine or DPPC-asparagine. Also, the liposomes were more stable in terms of aggregation or fusion than the others (DPPC-glutamine, DPPC-asparagine and DSPC-amino acids). As a rdsult, stable liposomes with an affinity for glucose could be prepared with DPPC and glutamic acid.

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Surface Properties of Liposomes Modified with Poly(ethylenimine) (폴리에틸렌이민으로 개질된 리포솜의 표면 특성)

  • 박윤정;남다은;서동환;한희동;김태우;김문석;신병철
    • Polymer(Korea)
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    • v.28 no.6
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    • pp.502-508
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    • 2004
  • Cationic liposomes for cancer treatment have been developed in the field of chemotharpy. It was well combined on the surface of anionic tumor cell membrane by electrostatic interaction. Thus, the object of this study was to prepare the cationic liposomes capable of forming an ionic complex with the anionic cell membrane. To prepare the cationic liposomes, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE) as a cationic lipid material and polyethylenimine (PEI) as a cationic polymer were synthesized. Ionic property on the surface of liposomes was determined by the zeta potential. The adsorption characteristics of plasma protein for liposome in bovine serum were determined by the particle size and turbidity change. To estimate the stability of liposome in buffered solution, the change of particle size was measured at room temperature for seven days. The cationic liposomes were absorbed a large amount of plasma protein in bovine serum because plasma protein having anionic charge was fixed on the surface of cationic liposomes. This result indicate that the modification on the surface of liposomes using cationic polyethylenimine enhances the protein adsorption in bovine serum. Additionaly, cationic liposomes showed good stability in buffered solution for seven days.

Ultrasound-Triggered Drug Release of Hydroxyapatite Coated Liposomes (하이드록시아파타이트 코팅 리포솜의 초음파에 의한 약물방출)

  • Cho, Sung Keun;Wee, Tae In;Ha, Jeung;Cho, Sun Hang;Han, Kun;Han, Hee Dong;Shin, Byung Cheol
    • Journal of the Korean Chemical Society
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    • v.57 no.4
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    • pp.493-498
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    • 2013
  • Liposomes, which can deliver payload at target site, have been studied as drug carrier. However, conventional liposomes have limitation for drug release at target site. Therefore, we developed hydroxyapatite (HA) coated ultrasound sensitive liposomes to increase drug release at target site and to enhance stability in blood stream. Control liposome was prepared using hydrogenated soy phosphatidylcholine (HSPC) and cholesterol, and then we assessed HA coating on the surface of control liposomes using calcium acetate, phosphoric acid, and 25% ammonium solution. Doxorubicin was used as a model drug. Size of HA coated liposomes was 120 nm and encapsulation efficiency of doxorubicin in liposomes was up to 95%. Size of HA coated liposomes are not changed in 30% serum solution, however, the control liposomes was 1.4 fold increased. After ultrasound triggered drug release from liposomes, intracellular efficiency of drug released from HA coated liposomes was 3 fold increased compared to control liposomes. In this study, we developed ultrasound sensitive liposomes to enhance drug release, which will be applied in controlled drug release at disease site.

Preparation of Protein-coated Cationic Liposomes Containing Doxorubicin and Their Binding Property of Blood Plasma Protein (독소루비신을 함유하고 단백질로 수식된 양이온성 리포솜의 제조 및 혈장 단백흡착 특성)

  • Kim, Sung-Kyu;Jung, Soon-Hwa;Jung, Suk-Hyun;Seong, Ha-Soo;Chi, Sang-Cheol;Cho, Sun-Hang;Shin, Byung-Cheol
    • Journal of the Korean Chemical Society
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    • v.52 no.1
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    • pp.57-65
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    • 2008
  • are nanometer or micrometer scale vesicles that can be used as drug delivery carriers. However, plain liposomes are plagued by rapid opsonization, making their circulation time in bloodstream be shortened. In this study, model protein, bovine serum albumin (BSA)-coated liposomes were prepared by coating cationic liposomes with BSA molecules at higher pH than isoelectric point of BSA. The BSA molecules coated on the liposomal surface were denatured by thermal treatment at above 60oC. While both plain and cationic liposomes had about mean particle diameter of 1041 nm, BSA-coated cationic liposomes (BCL) had mean particle diameter of 1091 nm. Encapsulation of model drug, doxorubicin (DOX), in liposomes were carried out by using remote loading method and the loading efficiency of DOX to liposomes was about 90%. The mean particle diameter of BCL did not increase in blood plasma and adsorption of plasma protein was much less than plain or cationic liposomes. These results suggest that BCL can be used as a long-circulating liposomes in bloodstream.

난용성 약물을 봉입한 리포솜의 장관혼수 기전연구

  • 김민수;정석재;심창구;이민화
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.279-279
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    • 1996
  • Sudan IV는 2시간 관류시키는 동안 약 30%의 농도감소를 보였다 Sudan IV자체는 물에 녹지않고 리포솜에 의해서 가용화 되는 물질이기 때문에 관류액중에서 리포솜으로부터 release out되지 않는다. 따라서 situation I의 가능성은 희박하며 또 그 자체로는 물에 거의 녹지않아 흡수되지 않을 것으로 예상되는 물질이므로 Sudan IV의 관류액으로부터의 소실은 곧바로 situation II를 반영할 것이다. 또 리포솜의 구성물질인 PC역시 관류액중에서 농도감소를 나타내었는데 이로부터 난용성약물을 봉입한 리포솜이 어떻게 장관으로 흡수되는 지 예상할 수 있었다.

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리포솜-아미노산 결합체의 제조와 포도당 민감성에 대한 연구

  • Mun, Je-Yeong;Lee, Gi-Yeong;Kim, Jin-Cheol;Park, Gi-Nam
    • 한국생물공학회:학술대회논문집
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    • 2000.11a
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    • pp.755-758
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    • 2000
  • Glucose sensitive liposomes-amino acid cinjugates Were prepared by DPPC and asparagine derivatives. Liposomes(amino acid added) have higher glucose binding affinity than liposome(amino acid non-added) or distilled water. The liposomes stabilily were increased by adding cholesterol. Liposomes(cholesterol non-added) particles size were bigger than cholesterol added liposomes.

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Preparation of Nano-liposome by Sonication and Pressure (초음파와 압력을 이용한 나노 리포솜의 제조)

  • Lee, Jung-Min;Cho, Yong-Jin;Park, Dong-Joon;Ko, Sung-Ho;Lee, Seung-Cheol
    • Korean Journal of Food Science and Technology
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    • v.40 no.1
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    • pp.115-117
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    • 2008
  • Liposomes are artificial membranes prepared by phospholipid. In this study, liposomes were prepared by dehydration-rehydration method, and then nano-sized by sonication and pressure. The sizes of the prepared multilamellar vesicles (MLV) were greater than 10 μm. Sonication with a tip-type sonifier or pressurization with a French press on MLV were carried out to reduce size. Sonication with an output of 112.5 W for 10 min on MLV resulted in sizes less than 450 nm. French press with 6,000 psi of pressure was able to manufacture liposomes of approximately 100 nm uniformly. Also, the sonication or pressure clarified the color of the liposome solutions. The results indicate that sonication and pressure via French press can be applied to obtain nano-sized liposomes.

Temperature-Dependent Release of Drug from Copolymers of N-Isopropylacrylamide Containing Liposome (리포솜이 함유된 N-이소프로필아크릴아마이드의 공중합체로부터 온도에 따른 약물의 방출)

  • 박영심;한희동;홍성욱;김승수;신병철
    • Polymer(Korea)
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    • v.28 no.1
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    • pp.59-66
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    • 2004
  • Thermosensitive poly(N-isopropylacrylamide) gels containing temperature-sensitive liposomes showing temperature-dependent sol-gel transition were prepared. The surface of temperature-sensitive liposome was modified with copolymers of N-isopropylacrylamide and octadecylacrylate, which exhibited a lower critical solution temperature at around 30 $^{\circ}C$ After mixing the modified temperature-sensitive liposomes with poly(N-isopropylacrylamide) solution, the temperature-sensitive 1iposomes formed physically cross-linked gels through heating the solution above their lower critical solution temperatures. The release of drug from temperature-sensitive liposomes was determined by measuring fluorescence intensity. The drug release from temperature-sensitive liposomes in poly(N-isopropylacrylamide) gel gradually showed sustained-release with increasing temperature.