Document Detail


Effect of nucleoside analogues and oligonucleotides on hydrolysis of liposomal phospholipids.
MedLine Citation:
PMID:  11058809     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The hydrolysis of the bilayer forming phospholipids resulting first of all in lysophospholipids and fatty acids is one limiting factor determining the shelf-life of liposomes. In several studies the influence of pH, buffer, lipid composition and other parameters on the hydrolysis of phospholipids have been demonstrated, but the influence of drugs has not yet been investigated systematically. In this study the influence of nucleoside analogues, especially 2', 2'-difluoro 2'-deoxycytidine (gemcitabine, dFdC) on the degradation of phospholipids was elucidated in more detail. It could be demonstrated that the interaction of dFdC with phospholipid bilayers promotes the hydrolysis of phospholipids in a concentration-dependent manner. Obviously two parts of the molecule, the amino group bound to the pyrimidine moiety and the 2', 2'-difluoro-2'-deoxyribose, seem to be responsible for the forced phospholipid hydrolysis. The dFdC-induced hydrolysis of phospholipids was influenced by pH, buffer, lipid composition and different anions. Optimization of the above parameters resulted in prolonged shelf-life of dFdC liposome dispersions, which is an important prerequisite for clinical practice.
Authors:
R Moog; M Brandl; R Schubert; C Unger; U Massing
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  206     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2000 Sep 
Date Detail:
Created Date:  2000-11-20     Completed Date:  2000-11-20     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  43-53     Citation Subset:  IM    
Affiliation:
Tumor Biology Center, Department of Clinical Research, Breisacher Strasse 117, 79106, Freiburg, Germany. reginam@farmasi.uit.no
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MeSH Terms
Descriptor/Qualifier:
Anions
Antimetabolites, Antineoplastic / administration & dosage
Buffers
Deoxycytidine / administration & dosage,  analogs & derivatives
Hydrogen-Ion Concentration
Hydrolysis
Lipid Bilayers / metabolism*
Liposomes
Lysophospholipids / administration & dosage*,  chemistry
Nucleosides / administration & dosage*,  chemistry
Oligonucleotides / administration & dosage*,  chemistry
Chemical
Reg. No./Substance:
0/Anions; 0/Antimetabolites, Antineoplastic; 0/Buffers; 0/Lipid Bilayers; 0/Liposomes; 0/Lysophospholipids; 0/Nucleosides; 0/Oligonucleotides; 103882-84-4/gemcitabine; 951-77-9/Deoxycytidine

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


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