Source:http://linkedlifedata.com/resource/pubmed/id/16819184
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
2006-7-4
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pubmed:abstractText |
We investigated the pharmacokinetic behavior of palmitoyl prednisolone (Pal-PLS) and its liposomes with L-alpha-distearoylphosphatidylcholine (DSPC) and cholesterol (Chol) with or without L-alpha-distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG 2000) after their intravenous administration in rats. Pal-PLS rapidly disappeared from the systemic circulation and prednisolone (PLS) was regenerated after the administration of DSPC/Chol liposomes. PEGylated liposomes including DSPE-PEG 2000, however, successfully maintained high blood concentrations of Pal-PLS and PLS. The blood profiles of drugs after the administration of liposomal Pal-PLS were analyzed according to a two-compartment model. The larger content of DSPE-PEG 2000 in DSPC/Chol liposomes showed a lower first order elimination rate constant from the central compartment (K(el)) and clearance (CL). The area under the concentration-time curve (AUC) of Pal-PLS and PLS in PEGylated liposomes was larger than DSPC/Chol liposomes. The mean resident time (MRT) of Pal-PLS and PLS was also prolonged by PEGylated liposomes. Although DSPC/Chol liposomes showed a high distribution of Pal-PLS in the liver and spleen, PEGylated liposomes significantly decreased the liver distribution of Pal-PLS. The biliary and urinary excretions of drugs for 240 min after drug administration were less than 1% of the administrated dose in any formulations. In conclusion, PEGylated liposomes, including Pal-PLS, are useful for maintain the PLS concentration in the blood after intravenous administration.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0918-6158
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
29
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1436-40
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16819184-Animals,
pubmed-meshheading:16819184-Bile,
pubmed-meshheading:16819184-Kinetics,
pubmed-meshheading:16819184-Liposomes,
pubmed-meshheading:16819184-Male,
pubmed-meshheading:16819184-Polyethylene Glycols,
pubmed-meshheading:16819184-Prednisolone,
pubmed-meshheading:16819184-Rats,
pubmed-meshheading:16819184-Rats, Wistar,
pubmed-meshheading:16819184-Tissue Distribution
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pubmed:year |
2006
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pubmed:articleTitle |
PEGylated liposomes loading palmitoyl prednisolone for prolonged blood concentration of prednisolone.
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pubmed:affiliation |
Department of Hospital Pharmacy, Nagasaki University Hospital of Medicine and Dentistry, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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