Liposomal entrapment of suramin.

H C Chang, D R Flanagan

文献索引：J. Pharm. Sci. 83(7) , 1043-6, (1994)

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摘要

The liposomal entrapment of suramin and similar compounds in phospholipid vesicles was examined. For dipalmitoylphosphatidylcholine (DPPC) liposomes, entrapment percentages ranged from 25 to 65% with 3-25 mM phospholipid for aqueous solutions containing 0.07 mM of suramin. Incorporation of 30-50 mol % cholesterol (CHL) into DPPC liposomes reduced the percentage suramin entrapment. Addition of positively-charged stearylamine (5 mol %) to DPPC/CHL liposomes increased the entrapment from 2.3% to 30.3%. Entrapment was not affected by the incorporation of negatively-charged phosphatidylglycerol into DPPC/CHL liposomes. When the amount of suramin was increased from 0.07 to 0.7 mM, the entrapment percentage decreased from 37% to 11% when DPPC was held constant at 6 mM. The entrapment of 0.07 mM Evans blue, a molecule similar in structure to suramin, was 51.6% in DPPC liposomes for 6 mM phospholipid. The entrapment percentage, however, decreased by about 50% when incorporated into 7:3 (DPPC/CHL) liposomes. The liposomal entrapment of disodium 1,5-naphthalenedisulfonic acid (5.5%) and sodium 3-amino-2,7-naphthalene-disulfonic acid (1.2%) was very low compared to that of suramin or Evans blue. Differential scanning calorimetry studies of suramin and an aqueous dispersion of DPPC showed an apparent interaction between them. These observations suggest that a significant portion of the entrapped suramin results from binding of suramin to the surface of or intercalation into the liposomal bilayer. Surface binding or intercalation into the phospholipid bilayer may be attributed to both ionic and hydrophobic interactions. The ionic interaction would arise from the suramin sulfonate groups associating with the cationic choline portion of the phospholipid.(ABSTRACT TRUNCATED AT 250 WORDS)