Development and in vitro evaluation of a novel lipid nanocapsule formulation of etoposide. - Université d'Angers Accéder directement au contenu
Article Dans Une Revue European Journal of Pharmaceutical Sciences Année : 2013

Development and in vitro evaluation of a novel lipid nanocapsule formulation of etoposide.

Benjamin Saliou
  • Fonction : Auteur
Olivier Thomas
  • Fonction : Auteur
  • PersonId : 1090470
Nolwenn Lautram
  • Fonction : Auteur
  • PersonId : 992808
José Hureaux
  • Fonction : Auteur
  • PersonId : 992806
Thierry Urban
  • Fonction : Auteur
  • PersonId : 1070062
Jean-Pierre Benoit
  • Fonction : Auteur
  • PersonId : 845448
Frédéric Lagarce
  • Fonction : Auteur
  • PersonId : 966544

Résumé

Small cell lung cancer (SCLC) is the most aggressive carcinoma in thoracic oncology, unfortunately, despite chemotherapy, relapse is constant. The effect of etoposide, a major drug used against SCLC, can potentially be enhanced after its encapsulation in nanocarriers. The aim of this study was to use the technology of lipid nanocapsules (LNCs) to obtain nanocarriers with drug loadings compatible with clinical use and with an industrial process. Solubility studies with different co-solvent were first performed, then several process were developed to obtain LNCs. LNCs were then characterized (size, zeta potential, and drug loading). The best formulation called Ω-LNCs had a size of 54.1±2.0 nm and a zeta potential of -5.8±3.5 mV and a etoposide drug loading of 5.7±0.3mg/g. The characteristics of this formulation were maintained after freeze drying and after a 15× scale-up. Release studies in a media mimicking plasma composition showed that 40% of the drug was released from the LNCs after 48 h. Moreover the activity of etoposide after encapsulation was enhanced on H209 cells, IC50 was 100 μM and 2.5 μM for etoposide and etoposide LNCs respectively. Unfortunately the formulation failed to be more cytotoxic than etoposide alone on H69AR cells that are resistant to etoposide. This study showed that is was possible to obtain a new etoposide nanocarrier without the use of organic solvent, that the process is suitable for scale-up and freeze drying and finally that etoposide activity is maintained which is very promising for future treatment of SCLC.

Fichier principal
Vignette du fichier
ejps-2013.pdf (1.13 Mo) Télécharger le fichier
Origine : Accord explicite pour ce dépôt

Dates et versions

hal-03171789 , version 1 (17-03-2021)

Identifiants

Citer

Benjamin Saliou, Olivier Thomas, Nolwenn Lautram, Anne Clavreul, José Hureaux, et al.. Development and in vitro evaluation of a novel lipid nanocapsule formulation of etoposide.. European Journal of Pharmaceutical Sciences, 2013, 50, pp.172-80. ⟨10.1016/j.ejps.2013.06.013⟩. ⟨hal-03171789⟩
11 Consultations
192 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More