Distribution of a lipidic 2.5 nm diameter dendrimer carrier after oral administration.
The biodistribution of a lipidic peptide dendrimer has been studied after oral administration to female Sprague-Dawley rats (180 g, 9 weeks old). Uptake by gut epithelial tissue of the radiolabelled dendrimer molecule (mol. wt. 6300; diameter 2.5 nm; log P=1.24) was studied in rats after a single oral dose by gavage (14 mg/kg). The maximum levels of dendrimer observed were 3% (blood), 1.5% (liver), 0.1% (spleen), 0.5% (kidneys), 15% (small intestine) and 5% (large intestine). Approximately 6% of a single administered dose (28 mg/kg) was recovered from the entire gastrointestinal tract while 1% was absorbed via the small intestine lymphoid tissue after 3 h; after 12 h, 0.1% was detected. The maximum uptake by the non-lymphoid small intestine was 4% of the dose after 3 h. After 12 h, 0.3 and 4% dendrimer was measured in the lymphoid large intestine and the non-lymphoid large intestine, respectively. The total percentage of the administered dose absorbed through the lymphoid tissue was comparatively greater than through the non-lymphoid tissue of the small intestine with respect to organ weight after 3 and 24 h.
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Centre for Drug Delivery Research, The School of Pharmacy, University of London, 29/39 Brunswick Square, London WC 1N 1AX, UK.
Toth
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Florence
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D000284:Administration, Oral; D000818:Animals; D004337:Drug Carriers / Q000493:pharmacokinetics*; D005260:Female; D007408:Intestinal Absorption; D008221:Lymphoid Tissue / Q000378:metabolism; D010455:Peptides / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley
D004337:Drug Carriers; D010455:Peptides