TY - JOUR
T1 - Jejunal Absorption, Pharmacological Activity, and Pharmacokinetic Evaluation of Indomethacin-Loaded Poly(d,l-Lactide) and Poly(Isobutyl-Cyanoacrylate) Nanocapsules in Rats
AU - Ammoury, Nazih
AU - Fessi, Hatem
AU - Devissaguet, Jean Philippe
AU - Dubrasquet, Marcelle
AU - Benita, Simon
PY - 1991/1
Y1 - 1991/1
N2 - The jejunal absorption of indomethacin nanocapsules was studied using an in vivo infusion technique. Jejunal absorption of indomethacin from the nanocapsules was slightly delayed as compared to a commercial indomethacin solution. The plasma and jejunal mucosa indomethacin concentrations were similar in both cases. However, the nanocapsules protected the rat jejunum from the ulcerating effect of indomethacin, probably by avoiding direct contact of the free drug with the surface of the mucosa. The pharmacokinetic profile of indomethacin nanocapsule formulations was compared to a solution of free drug following oral administration of 5 mg/kg in rats; no difference in the mean concentration–time profiles of the drug was observed. Blood levels of thromboxane showed a sustained biological activity, over a period of 24 hr, of indomethacin-loaded nanocapsules, relative to the drug in solution, following oral administration.
AB - The jejunal absorption of indomethacin nanocapsules was studied using an in vivo infusion technique. Jejunal absorption of indomethacin from the nanocapsules was slightly delayed as compared to a commercial indomethacin solution. The plasma and jejunal mucosa indomethacin concentrations were similar in both cases. However, the nanocapsules protected the rat jejunum from the ulcerating effect of indomethacin, probably by avoiding direct contact of the free drug with the surface of the mucosa. The pharmacokinetic profile of indomethacin nanocapsule formulations was compared to a solution of free drug following oral administration of 5 mg/kg in rats; no difference in the mean concentration–time profiles of the drug was observed. Blood levels of thromboxane showed a sustained biological activity, over a period of 24 hr, of indomethacin-loaded nanocapsules, relative to the drug in solution, following oral administration.
KW - indomethacin
KW - intestinal lesions
KW - jejunal absorption
KW - oral pharmacokinetics
KW - polymeric nanocapsules
KW - thromboxane
UR - http://www.scopus.com/inward/record.url?scp=0026017143&partnerID=8YFLogxK
U2 - 10.1023/A:1015846810474
DO - 10.1023/A:1015846810474
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C2 - 2014197
AN - SCOPUS:0026017143
SN - 0724-8741
VL - 8
SP - 101
EP - 105
JO - Pharmaceutical Research
JF - Pharmaceutical Research
IS - 1
ER -