International journal of pharmaceutics
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The purpose of this study was to investigate the effect of morin on the pharmacokinetics of orally and intravenously administered paclitaxel in rats. Pharmacokinetic parameters of paclitaxel were determined in rats after an oral (30 mg kg(-1)) or intravenous (3 mg kg(-1)) administration of paclitaxel to rats in the presence and absence of morin (3.3 and 10 mg kg(-1)). Compared to the control given paclitaxel alone, pretreatment with morin 30 min prior to the oral administration of paclitaxel increased C(max) and AUC of paclitaxel by 70-90% and 30-70%, respectively, while there was no significant change in T(max) and terminal plasma half-life (T(1/2)) of paclitaxel. ⋯ In contrast, following an intravenous administration of paclitaxel (3.3 mg kg(-1)), the pharmacokinetic profiles of paclitaxel were not altered significantly in the presence of morin. Those results suggest that the enhanced oral exposure of paclitaxel should be mainly due to the inhibition effect of morin on the gastrointestinal extraction of paclitaxel during the intestinal absorption. Therefore, the concurrent use of morin or morin-containing dietary supplement may provide a therapeutic benefit in the oral delivery of paclitaxel.
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Glyceryl monooleate (GMO) is a polar amphiphilic lipid, which forms different sequential lyotropic liquid crystals upon hydration. GMO has been utilized for various delivery systems and routes of administrations. Owing to sticky and waxy nature of GMO, preparation of oral solid dosage form utilizing GMO is still a challenge for pharmaceutical researchers. ⋯ The drug released from powder precursor was initially governed by the cubic phase formed and in later stage it depends upon dynamic swelling behavior of hexagonally packed cylindrical aggregates. The drug loaded powder precursor was found to have more effective and prolonged anti-inflammatory and analgesic activity as compared to pure drug. Thus the dry powder precursor of cubic phase was prepared in which drug release was entirely governed by the mesophases formed.