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Amidine-bearing lipoplex targeting to hepatocyte cells

Chinese Chemical Letters 2008年第9期19卷 1115-1118页

作者： Yasuya Kudo Kazunori Koiwai Kazuhiro Shimizu Shota Kusuki mina sakuragi Naohiko Shimada Yoichi Takeda Kazuo Sakurai Department of Chemical Process & Environments Faculty of Environmental EngineeringThe University of Kitakyushu1-1HibikinoWakamatsu-kuKitakyushuFukuoka 808-0135Japan TERUMO Corporation R & D Center 1500 InokuchiNakai-machiAshigarakami-gun Kanagawa 259-0151Japan

A lipoplex （i.e., pDNA#1/lipid complex and transfection reagent for pDNA delivery） containing galactosylceramide （GalCer） and an amidine-bearing lipid （TRX） was examined whether the bound pDNA was specifically ingested by hepatocyte via asialoglycoprotein receptor （ASGPR） and then expressed protein. Gel electrophoresis and small-angle X-ray scattering （SAXS） confirmed that the TRX-GalCer liposome#2 complexed with pDNA and the resultant lipoplex took a hexagonally packed inverted cylinder structure when the GalCer composition was less than 20 wt.% of the total lipid. When the lipoplex carrying pGL3 （luciferase-cording pDNA） was administrated to HepG2, the luciferase activity was increased with increasing the GalCer composition until it reached 3 wt.% and then decreased upon further addition of GalCer. When we added galactose itself as a competitor, the luciferase activity was decreased, while glucose did not show such decrease, suggesting that HepG2 ingested the lipoplex via ASGPR-mediated endocytosis. This paper indicated that the hexagonally packed inverted cylinder structures of lipoplex may not always provide excellent transfection and presented a possibility that the TRX lipoplex#3 can obtain a cellulartargeting ability through the receptors for oligosaccharide.

关键词： Gene theraphy Amidine Galactosylceramide Targeting

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Effect of PEGylation on the physicochemical and pharmacokinetic characteristics of bovine serum albumin-encapsulated liposome

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Asian Journal of Pharmaceutical Sciences 2016年第1期11卷 112-113页

作者： Yuko Okamoto Kazuaki Taguchi Keishi Yamasaki mina sakuragi Shun’ichi Kuroda Masaki Otagiri Faculty of Pharmaceutical Sciences Sojo UniversityKumamoto 860-0082Japan Department of Nanoscience Sojo UniversityKumamoto 860-0082Japan The Institute of Scientific and Industrial Research Osaka UniversityOsaka 567-0047Japan Graduate School of Bioagricultural Sciences Nagoya UniversityNagoya 464-8601Japan

There is now little doubt that PEGylation is useful and is in widespread use because it provides a prolonged half-life,a higher stability and a lowerimmunogenicity[1].However,it is of concern that PEGylation may affect the physicochemical and pharmacokinetic characteristics of protein-encapsulated ***,we prepared the bovine serum albumin(BSA)-encapsulated liposome(BSA-liposome)with or without PEG and then compared their physicochemical and pharmacokinetic characteristics(Fig.1).BSA-liposomes were prepared by the thin-film hydration method.

关键词： Liposome PEGylation Bovine serum albumin

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