Nanoparticles loaded with ferrocenyl tamoxifen derivatives for breast cancer treatment. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue International Journal of Pharmaceutics Année : 2008

Nanoparticles loaded with ferrocenyl tamoxifen derivatives for breast cancer treatment.

Résumé

For the first time, two organometallic triphenylethylene compounds (Fc-diOH and DFO), with strong antiproliferative activity in breast cancer cells, but insoluble in biological fluids, were incorporated in two types of stealth nanoparticles (NP): PEG/PLA nanospheres (NS) and nanocapsules (NC). Their physicochemical parameters were measured (size, zeta potential, encapsulation and loading efficiency), and their biological activity was assessed. In vitro drug release after high dilution of loaded NPs was measured by estradiol binding competition in MELN cells. The influence of the encapsulated drugs on the cell cycle and apoptosis was studied by flow cytometry analyses. Notwithstanding potential drug adsorption at the NP surface, Fc-diOH and DFO were incorporated efficiently in NC and NS, which slowly released both compounds. They arrested the cell cycle in the S-phase and induced apoptosis, whose activity is increased by loaded NS. A decrease in their antiproliferative activity by the antioxidant alpha-tocopherol indicated that reactive oxygen species (ROS) may be involved. Therefore, nanosystems, containing for the first time a high load of anticancer organometallic triphenylethylenes, have been developed. Their small size and delayed drug release, combined with their enhanced apoptotic potential, are compatible with an increased persistence in the blood and a promising antitumour activity.
Fichier principal
Vignette du fichier
Nanoparticles loaded with.pdf (307.9 Ko) Télécharger le fichier
Origine : Fichiers produits par l'(les) auteur(s)
Loading...

Dates et versions

hal-00180710 , version 1 (20-11-2019)

Identifiants

Citer

Anh Nguyen, Véronique Marsaud, Céline Bouclier, Siden Top, Anne Vessieres, et al.. Nanoparticles loaded with ferrocenyl tamoxifen derivatives for breast cancer treatment.. International Journal of Pharmaceutics, 2008, 347 (1-2), pp.128-35. ⟨10.1016/j.ijpharm.2007.06.033⟩. ⟨hal-00180710⟩
205 Consultations
125 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More