Document Detail


Liposomal entrapment of suramin(II): interaction of suramin with phospholipids of various chain lengths.
MedLine Citation:
PMID:  8537885     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Previously, we reported that the entrapment of suramin in dipalmitoylphosphatidylcholine (DPPC, C16) multilamellar liposomes ranged from 25% to 65% and the addition of 30-50 mol% cholesterol (CHL) greatly reduced entrapment. Entrapment of small molecules similar to suramin, disodium 1,5-naphthalenedisulfonic acid (5.5%) and sodium 3-amino-2,7-naphthalenedisulfonic acid (1.2%), were very low. In the present study, the entrapment and interaction of suramin with dilauroylphosphatidylcholine (DLPC, C12), dimyristoylphosphatidylcholine (DMPC, C14), and distearoylphosphatidylcholine (DSPC, C18) liposomes was investigated. DLPC and DMPC showed 2-3-fold higher entrapment percentages (95.1% and 74.2%, respectively) than DPPC (37%). However, the entrapment with DSPC (29%) was about 25% lower than DPPC. Adding 50 mol% cholesterol greatly reduced suramin entrapment for all phospholipids. The entrapment of polysulfonated dyes such as Evans blue, Direct blue 1, or Trypan blue, which are structurally similar to suramin, was found to be in the same order of DLPC > DMPC > DPPC > DSPC. Differential scanning calorimetry of aqueous dispersions of DLPC and DMPC with suramin showed more apparent interaction than for DPPC and DSPC. These results suggest that a large portion of the associated suramin and other polysulfonated compounds results from binding to the surface of the phospholipid bilayer or intercalation into the liposomal bilayer. The phospholipid chain length effect on entrapment may be due to the lower net van der Waals interaction between hydrocarbon chains for shorter acyl chains which also increases the bilayer intermolecular spacing. Such effects could then increase the ability of suramin to interact with individual phospholipid molecules.
Authors:
H C Chang; D R Flanagan
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  84     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1995 Sep 
Date Detail:
Created Date:  1996-02-05     Completed Date:  1996-02-05     Revised Date:  2006-04-17    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1078-82     Citation Subset:  IM    
Affiliation:
Division of Pharmaceutics, College of Pharmacy, University of Iowa, Iowa City 52242, USA.
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MeSH Terms
Descriptor/Qualifier:
Azo Compounds / chemistry
Calorimetry, Differential Scanning
Coloring Agents
Evans Blue
Liposomes
Membranes, Artificial
Phospholipids
Suramin / administration & dosage*,  chemistry
Temperature
Trypan Blue
Chemical
Reg. No./Substance:
0/Azo Compounds; 0/Coloring Agents; 0/Liposomes; 0/Membranes, Artificial; 0/Phospholipids; 145-63-1/Suramin; 2610-05-1/pontamine sky blue; 314-13-6/Evans Blue; 72-57-1/Trypan Blue

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