[Influence of soybean-derived sterylglucoside and amphipathic polyethylene glycol on the cellular delivery and anisotropy of different cationic liposomes].
OBJECTIVE
To investigate the influences of different lipids on cellular delivery and fluidity of liposome membrane of cationic liposome.


METHODS
The 3 beta [N-(N',N'-dimethylaminoethane) carbamoyl] cholesterol (DC-chol), a cationic lipid was synthesized, which is approved by FDA. Using fluorescein sodium (SF) as a model material, dipalmitoylphosphatidylcholine (DPPC), dioleoylphosphatidylethanolamine (DOPE) and cholesterol (ch) as help lipids, the DPPC/ch/DC-chol cationic liposomes, DOPE/ch/DC-chol cationic liposome and soybean-derived sterylglucoside (SG) or polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) modified cationic liposomes were prepared, respectively. The neutral liposome DPPC/ch was also prepared. HepG2 2.2.15 was selected as an in vitro cell culture assay model to investigate the cellular delivery of different liposomes. The influences of different lipids on the fluidity of liposome membranes were investigated with the technique of fluorescence polarization.


RESULTS
It is showed that the DC-chol has significant influences on the incorporation efficiencies (from 0.64% to 74.84%), cellular delivery (from 1.83% to 32.29%) and the fluidity of liposome membrane; SG can significantly increase the incorporation efficiency (from 52.60% to 63.37%), cellular delivery (from 20.18% to 47.48%) and fluidity of liposome membrane; PEG-DSPE can enhance the cellular delivery of cationic liposome (from 20.18% to 28.17%).


CONCLUSIONS
DC-chol and SG can significantly increase the cellular delivery and fluidity of liposome membrane, PEG-DSPE can enhance the cellular delivery of cationic liposome.
Yan
Wenwei
W
Department of Pharmaceutics, Peking University School of Pharmaceutical Science, Beijing 100083, China.
Fei
Ran
R
Wang
Wenhao
W
Qi
Xianrong
X
Wei
Lai
L
Cong
Xu
X
Wang
Yu
Y
D016880:Anisotropy; D002460:Cell Line; D002782:Cholestenes / Q000494:pharmacology*; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry*; D008560:Membrane Fluidity; D011092:Polyethylene Glycols / Q000494:pharmacology*; D013025:Glycine max / Q000737:chemistry*; D014162:Transfection
D002782:Cholestenes; D008081:Liposomes; C096056:soy derived sterylglucoside mixture; D011092:Polyethylene Glycols