Document Detail

pH-sensitive, serum-stable and long-circulating liposomes as a new drug delivery system.
MedLine Citation:
PMID:  11829129     Owner:  NLM     Status:  MEDLINE    
The lack of stability in blood and the short blood circulation time of pH-sensitive liposomes are major drawbacks for their application in-vivo. To develop pH-sensitive, serum-stable and long-circulating liposomes as drug delivery systems, the impact of polyethylene glycol-derived phosphatidylethanolamine (DSPE-PEG) on the properties of pH-sensitive liposomes was investigated. pH-sensitive liposomes were prepared with dioleoylphosphatidylethanolamine (DOPE) and oleic acid (DOPE/oleic acid liposome) or DOPE and 1,2-dipalmitoylsuccinylglycerol (DOPE/DPSG liposome). The inclusion of DSPE-PEG enhanced the serum stability of both DOPE/oleic acid and DOPE/DPSG liposomes, but also shifted the pH-response curve of pH-sensitive liposomes to more acidic regions and reduced the maximum leakage percentage. The impact of DSPE-PEG, however, was much lower in the DOPE/DPSG liposomes than in the DOPE/oleic acid liposomes. In tumour tissue homogenates, where the pH is lower than normal healthy tissues, the pH-sensitive DOPE/DPSG liposomes released the entrapped markers rapidly, in comparison with pH-insensitive dipalmitoylphosphatidylcholine/cholesterol/DSPE-PEG liposomes. Moreover, the release rate was not affected by the content of DSPE-PEG. The blood circulation time of methotrexate incorporated in DOPE/UDPSG liposomes was significantly prolonged with increasing content of DSPE-PEG. Taken together, the liposomes composed of DOPE, DPSG and DSPE-PEG (up to 5%) were pH sensitive, plasma stable and had a long circulation time in the blood. The complete destabilization of the liposomes at tumour tissues suggests that the liposomes might be useful for the targeted delivery of drugs such as anticancer agents.
Myo-Sook Hong; Soo-Jeong Lim; Yu-Kyoung Oh; Chong-Kook Kim
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  54     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  2002 Jan 
Date Detail:
Created Date:  2002-02-06     Completed Date:  2002-07-17     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  51-8     Citation Subset:  IM    
College of Pharmacy, Seoul National University, Kwanak-Gu, South Korea.
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MeSH Terms
Analysis of Variance
Area Under Curve
Drug Delivery Systems*
Drug Stability
Enzyme Inhibitors / administration & dosage*,  pharmacokinetics
Hydrogen-Ion Concentration
Methotrexate / administration & dosage*,  pharmacokinetics
Mice, Inbred C57BL
Phosphatidylethanolamines / pharmacology
Polyethylene Glycols / pharmacology
Rats, Sprague-Dawley
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Liposomes; 0/Phosphatidylethanolamines; 0/Polyethylene Glycols; 4537-76-2/1,2-distearoylphosphatidylethanolamine; 59-05-2/Methotrexate

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