Drug delivery to tumours using a novel 5-FU derivative encapsulated into lipid nanocapsules - CNRS - Centre national de la recherche scientifique Accéder directement au contenu
Article Dans Une Revue Journal of Drug Targeting Année : 2019

Drug delivery to tumours using a novel 5-FU derivative encapsulated into lipid nanocapsules

Kevin Matha
Thomas Dehoux
Jean-Paul Rieu
Thomas Perrier
  • Fonction : Auteur
  • PersonId : 780401
  • IdRef : 080800653

Résumé

In this work, a novel lipophilic 5-fluorouracil (5-FU) derivative was synthesised and encapsulated into lipid nanocapsules (LNC). 5-FU was modified with lauric acid to give a lipophilic mono-lauroyl-derivative (5-FU-C12, MW of about 342 g/mol, yield of reaction 70%). 5-FU-C12 obtained was efficiently encapsulated into LNC (encapsulation efficiency above 90%) without altering the physico-chemical characteristics of LNC. The encapsulation of 5-FU-C12 led to an increased stability of the drug when in contact with plasma being the drug detectable until 3 h following incubation. Cytotoxicity assay carried out using MTS on 2D cell culture showed that 5-FU-C12-loaded LNC had an enhanced cytotoxic effect on glioma (9L) and human colorectal (HTC-116) cancer cell line in comparison with 5-FU or 5-FU-C12. Then, HCT-116 tumour spheroids were cultivated and the reduction of spheroid volume was measured following treatment with drug-loaded LNC and drugs alone. Similar reduction on spheroids volume was observed following the treatment with drug-loaded LNC, 5-FU-C12 and 5-FU alone, while blank LNC displayed a reduction in cell viability only at high concentration. Globally, our data suggest that the encapsulation increased the activity of the 5-FU-C12. However, in-depth evaluations of LNC permeability into spheroids are needed to disclose the potential of these nanosystems for cancer treatment.
Fichier principal
Vignette du fichier
preprint.pdf (1.06 Mo) Télécharger le fichier
Origine : Fichiers produits par l'(les) auteur(s)
Loading...

Dates et versions

hal-02996676 , version 1 (09-11-2020)

Identifiants

Citer

Giovanna Lollo, Kevin Matha, Martina Bocchiardo, Jérôme Bejaud, Ilaria Marigo, et al.. Drug delivery to tumours using a novel 5-FU derivative encapsulated into lipid nanocapsules. Journal of Drug Targeting, 2019, 27 (5-6), pp.634-645. ⟨10.1080/1061186X.2018.1547733⟩. ⟨hal-02996676⟩
120 Consultations
422 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More