Cationic liposomes are known to be useful tools for gene transfection. However, the relation between transfection efficiency and physicochemical properties of liposomes has not been well understood. Here, we synthesized eight cationic derivatives of cholesterol which contain a tertiary amino head group with a different spacer arm. Transfection of plasmid pSVZCAT DNA into cells was done by cationic liposomes made of a mixture of dioleoylphosphatidylethanolamine (DOPE) and each cationic cholesterol derivative. At the same time we measured zeta potential of cationic liposomes by laser Doppler spectroscopy. The present results indicated that zeta potentials of cationic liposomes were well related to transfection activity of pSV2CAT DNA. This suggested that zeta potential of cationic liposomes is one of important factors which control gene transfection.
SummaryVarious molar ratios of the constituents of sulfatidecontaining liposomes (egg phosphatidylcholine, cholesterol, and sulfatide) were examined with respect to liposomal efficiency to entrap adriamycin (ADM) and to the tissue distribution. Among the ratios of the constituents examined, 5 : 4 : 1 was the best in terms of entrapment efficiency for both multilamellar vesicles (MLV) and small unilamellar vesicles (SUV). Tissue distribution studies of liposome-entrapped ADM showed that the blood clearance and cardiac uptake of ADM were significantly reduced when the drug was entrapped in the above liposomes, especially in the MLV; Incorporation of ADM into ovarian tumors transplanted into nude mice was increased when the drug was entrapped in the SUV.
The effect of y-Oryzanol, ferulic acid esters obtained from rice oil, on climacteric disturbances was studied with special reference to lipid peroxide levels in the sera of patient. 300 mg of y-Oryzanol was administered daily to each patient for 4 to 8 weeks. In 85% of 40 cases the effect on the climacteric disturbance was judged by the Kupperman method to be significant. In patients with climacteric disturbances, serum lipid peroxide levels were high, but were reduced significantly after administration of y-Oryzanol. By its administration, total cholesterol, triglyceride and HDLcholesterol were improved in cases with hyperlipidemia (TC>220 mg/dl, TG>140 mg/dl, HDL-chol.<45 mg/dl). The atherogenic index was also considerably reduced. No side effects and n o particular changes in functional tests were observed.
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