Source:http://linkedlifedata.com/resource/pubmed/id/15664130
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1-2
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pubmed:dateCreated |
2005-1-24
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pubmed:abstractText |
Conventional lipid microspheres (LM) were prepared using soybean oil and lipid at a 5.5:1 weight ratio with lipid phase consisting of PC (phosphatidyl choline):CH (cholesterol) (1:0.5) by molar ratio. The average diameter of the particles was 150 nm. Long-circulating microspheres (S-LM) were also prepared similarly but the lipid phase consisted of PC:CH:DSPE-PEG (phosphatidyl choline:cholesterol:distearoyl phosphatidyl ethanolamine-polyethylene glycol) 1:0.5:0.16 by molar ratio. A comparative biodistribution study was conducted between free indomethacin and lipo-indomethacin (LM and S-LM) in the arthritic rats by administering the formulations at a dose equivalent to 12 mg of indomethacin/kg. It was observed that the free drug as well as the encapsulated drug followed biphasic clearance from the blood. Pharmacokinetic parameters, such as AUC(0-t), terminal half-life, MRT increased significantly when the drug was used in encapsulated form (p < 0.05). Clearance of the drug was reduced 1.4 times with the conventional lipid microspheres and was reduced three-fold when encapsulated in polyethylene glycol-coated lipid microspheres. The overall drug targeting efficiency (T(e)) with the PEG-coated lipid microspheres was 7.5-fold higher than the conventional lipid microspheres. The high accumulation of the drug in arthritic paw with S-LM system may be accounted for by the reduced uptake by RES cells, and thereby, availability for extravascularization in the inflammatory tissues.
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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 |
Feb
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pubmed:issn |
0378-5173
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
290
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
55-62
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15664130-Animals,
pubmed-meshheading:15664130-Arthritis, Experimental,
pubmed-meshheading:15664130-Biological Availability,
pubmed-meshheading:15664130-Indomethacin,
pubmed-meshheading:15664130-Liposomes,
pubmed-meshheading:15664130-Male,
pubmed-meshheading:15664130-Microspheres,
pubmed-meshheading:15664130-Polyethylene Glycols,
pubmed-meshheading:15664130-Rats,
pubmed-meshheading:15664130-Rats, Wistar,
pubmed-meshheading:15664130-Tissue Distribution
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pubmed:year |
2005
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pubmed:articleTitle |
Biodisposition of PEG-coated lipid microspheres of indomethacin in arthritic rats.
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pubmed:affiliation |
College of Pharmacy, South Dakota State University, Brookings, SD 57007, USA. Srinath_palakurthi@sdstate.edu
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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