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1.
Chem Biodivers ; 20(8): e202300534, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37498138

RESUMO

Olive leaf extract is a valuable source of phenolic compounds; primarily, oleuropein (major component) and rutin. This natural olive leaf extract has potential use as a therapeutic agent for cancer treatment. However, its clinical application is hindered by poor pharmacokinetics and low stability. To overcome these limitations, this study aimed to enhance the anticancer activity and stability of oleuropein and rutin by loading them into PEGylated Nano-phytosomes. The developed PEGylated Nano-phytosomes exhibited favorable characteristics in terms of size, charge, and stability. Notably, the anticolonic cancer activity of the Pegylated Nano-phytosomes loaded with oleuropein (IC50=0.14 µM) and rutin (IC50=0.44 µM) surpassed that of pure oleuropein and rutin alone. This outcome highlights the advantageous impact of Nano-phytosomes to augment the anticancer potential of oleuropein and rutin. These results present a promising pathway for the future development of oleuropein and rutin Nano-phytosomes as effective options for passive tumor-targeted therapy, given their improved stability and efficacy.


Assuntos
Neoplasias , Olea , Rutina/farmacologia , Antioxidantes , Iridoides/farmacologia , Glucosídeos Iridoides , Polietilenoglicóis , Folhas de Planta , Extratos Vegetais/farmacologia
2.
Int J Pharm ; 311(1-2): 63-8, 2006 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-16455214

RESUMO

The pharmacokinetic parameters, i.e. peak concentration (c(max)); peak time (t(max)); area under the curve (AUC); elimination rate constant (k); absorption rate constant (k(a)); Drug clearance (cl(t)), and the volume of distribution (v(d)) of sodium salicylate administered in fractionated coconut oil (FCO) have been compared with that from an aqueous and glycerin vehicles using a three-way crossover study in 12 rabbits. The results of the study show that all of the pharmacokinetic parameters tested differ significantly when administered in oily rather than aqueous or glycerin vehicles. No statistically significant difference was found between any of the above mentioned parameters when comparison was made between aqueous and glycerin formulations. The results indicate that sodium salicylate is absorbed at a lower rate but to a greater extent from oily formulation. Possible reasons for these differences are discussed and is suggested, therefore, that the oily formulation might be used as a sustained release preparation.


Assuntos
Anti-Inflamatórios não Esteroides/farmacocinética , Veículos Farmacêuticos , Óleos de Plantas/química , Salicilato de Sódio/farmacocinética , Água/química , Administração Oral , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Química Farmacêutica , Óleo de Coco , Esvaziamento Gástrico/efeitos dos fármacos , Trânsito Gastrointestinal/efeitos dos fármacos , Glicerol/química , Absorção Intestinal/efeitos dos fármacos , Masculino , Óleos de Plantas/farmacologia , Coelhos , Salicilato de Sódio/administração & dosagem , Salicilato de Sódio/química , Viscosidade
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