Document Detail

Characterization of distribution behavior of 2-imidazolines into multilamellar liposomes.
MedLine Citation:
PMID:  1791536     Owner:  NLM     Status:  MEDLINE    
The distribution of 2-imidazolines in neutral dimyristoylphosphatidylcholine (DMPC) liposomes, in negatively charged liposomes containing dicetylphosphate (DCP) or phosphatidylserine (PS), and in positively charged liposomes containing stearylamine (STA), has been investigated. Electrophoretic mobilities of multilamellar liposomes have also been measured as a function of drug concentration. Apparent equilibrium partition coefficients (log K'm) increased as a function of the DCP or PS concentration in DMPC liposomes whereas log K'm decreased with STA concentration, except for lofexidine and clonidine. Similarly, the electrokinetic parameters increased in DMPC liposomes that exhibited a small, positive surface charge, decreased in DMPC/cholesterol/DCP (7:1:2 mole ratio) liposomes, and increased in DMPC/STA (3:1 mole ratio) liposomes, except for clonidine which showed a decrease, as a function of the 2-imidazoline concentration. Surface potential change (delta psi o) due to drug inclusion in the liposomes obtained from theoretical considerations exhibited a positive linear relationship with log K'm. Values of delta psi o were greater but less sensitive to log K'm in negatively charged than in neutral or positively charged liposomes at 1 mM drug concentration. Likewise, surface charge densities varied in the same order as the surface potentials as a function of log K'm of the 2-imidazolines, except for clonidine and lofexidine. These data indicate the relative importance of the membrane surface characteristics on the partitioning behavior, and also possibly the membrane transport behavior, of the 2-imidazoline drugs.
Y W Choi; J A Rogers
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  80     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1991 Aug 
Date Detail:
Created Date:  1992-04-01     Completed Date:  1992-04-01     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  757-60     Citation Subset:  IM    
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada.
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MeSH Terms
Amines / chemistry
Chemistry, Physical
Dimyristoylphosphatidylcholine / chemistry
Drug Carriers
Hydrogen-Ion Concentration
Imidazoles / chemistry*
Liposomes / chemistry
Phosphatidylserines / chemistry
Physicochemical Phenomena
Reg. No./Substance:
0/Amines; 0/Drug Carriers; 0/Imidazoles; 0/Liposomes; 0/Phosphatidylserines; 124-30-1/stearylamine; 13699-48-4/Dimyristoylphosphatidylcholine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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