Prolongation of Liposome Circulation Time by Various Derivatives of Polyethyleneglycols
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概要
- 論文の詳細を見る
New lipid derivatives of polyethyleneglycol (PEG) have been synthesized and tested for the ability to allow liposomes to evade uptake by the reticuloendothelial system (RES) and to prolong the circulation time of liposomes in mice. Liposomes were prepared from distearoylphosphatidylcholine (DSPC) and cholesterol (CH) (1 : 1,m/m) containing 6 mol% of various PEG-derivatives. The activity of the CH derivative of PEG (CH-PEG) in prolonging the circulation time of liposomes was proportional to the average molecular weight of PEG, i.e., 4800>2600>1700>800. α-Methoxy-ω-(1,2-dioctadecenoyloxy glyceryl)polyoxyethylene (DO-PEG) 1000 and α-methoxy-ω-(1,2-ditetradecenoyloxy glyceryl) polyoxyethylene (DT-PEG) 1000,in which PEG is directly linked to glycerol, prolonged the circulation time as effectively as distearoylphosphatidyl-N-(methoxy polyoxyethylene succinyl)-ethanolamine (DSPE-PEG). PEG-derivatives with a functional group at the PEG terminal, such as distearoyl-phosphatidyl-N-(3-carboxypropionyl polyoxyethylene succinyl)ethanolamine (DSPE-PEG-COOH) and α-(dipalmi-toylphosphatidyl)-ω-hydroxypolyoxyethylene (DPP-PEG-OH), effectively prolonged the circulation time of liposomes. incorporation of PEG-derivatives did not change membrane fluidity even after treatment with serum. Furthermore, Incorporation of PEG-derivatives into liposomes decreased uptake by J774 cells, a murine macrophage-like cell line, in vitro. The newly synthesized PEG-derivatives seem to prevent or reduce the interactions of liposomes with serum protein and macrophages, resulting in enhanced stability and a prolonged circulation time.
- 社団法人日本薬学会の論文
- 1996-10-15
著者
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Maruyama K
帝京大学 薬 薬剤
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YUDA Tsutomu
Faculty of Pharmaceutical Sciences, Teikyo University
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MARUYAMA Kazuo
Faculty of Pharmaceutical Sciences, Teikyo University
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IWATSURU Motoharu
Faculty of Pharmaceutical Sciences, Teikyo University
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Yuda Tsutomu
Faculty Of Pharmaceutical Sciences Teikyo University
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Iwatsuru Motoharu
Faculty Of Pharmaceutical Sciences Teikyo University
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Maruyama Kazuo
Faculty Of Pharmaceutical Sciences Kumamoto University
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Iwatsuru M
Teikyo Univ. Kanagawa
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Maruyama Kazuo
Faculty of Engineering, Niigata University
関連論文
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- Preparation of Thermosensitive Liposomes for Macromolecule Delivery
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