Indomethacinterpenoids' esters (1–4) were synthesized and assessed both in vitro and in vivo as indomethacindermalprodrugs. Esters 1–4 showed high lipophilicity, poor water solubility, good stability in hydro-alcoholic medium (ethanol/water 1:1) and rapid enzymatic cleavage. Results from in vitro percutaneous absorption studies showed that esters 1 and 2 slightly increased the cumulative uptake of indomethacin through excised human skin compared with the parent drug. In vivo results, using methyl nicotinate (MN) induced erythema as an inflammatory model in human volunteers, showed an interesting delayed and sustained activity of ester 1 compared with the parent drugs.
In vitro and in vivo evaluation of terpenoid esters of indomethacin as dermal prodrugs
DE CAPRARIIS, Paolo
1997-01-01
Abstract
Indomethacinterpenoids' esters (1–4) were synthesized and assessed both in vitro and in vivo as indomethacindermalprodrugs. Esters 1–4 showed high lipophilicity, poor water solubility, good stability in hydro-alcoholic medium (ethanol/water 1:1) and rapid enzymatic cleavage. Results from in vitro percutaneous absorption studies showed that esters 1 and 2 slightly increased the cumulative uptake of indomethacin through excised human skin compared with the parent drug. In vivo results, using methyl nicotinate (MN) induced erythema as an inflammatory model in human volunteers, showed an interesting delayed and sustained activity of ester 1 compared with the parent drugs.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
