In vivo evaluation of paclitaxel-loaded lipid nanocapsules after intravenous and oral administration on resistant tumor.

Anne-Claire Groo (1) , M Bossière (1) , L Trichard (2) , Pierre Legras (3) , Jean-Pierre Benoît (1) , Frédéric Lagarce (1)

1 MINT - Micro et Nanomédecines Biomimétiques
2 Novosibirsk State University,
3 SCAHU - Service Commun Animalerie hospitalo-universitaire

UNLABELLED: Aim & methods: The aim of the present work was to encapsulate paclitaxel (Ptx) in various lipid nanocapsules (LNCs) formulations and then to compare their pharmacokinetics and efficacy on a subcutaneous isograft model in rats.

RESULTS: Three different Ptx formulations were obtained. Drug payloads ranged from 1.32 to 3.62 mg Ptx/g of formulation. After oral administration the area under concentration-time curve was higher (p < 0.05) if Ptx was encapsulated, (1,2 Distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(PEG)] (DSPE-PEG-NH2)) LNCs displaying the highest area under concentration-time curve (p < 0.05). Efficacy was better than control for standard LNCs after oral administration (p < 0.05) and for (DSPE-PEG-NH2) LNCs after intravenous administration. Despite good absorption, (DSPE-PEG-NH2) LNCs failed to remain efficient after oral route.

CONCLUSION: This study highlights the importance of efficacy studies paired to pharmacokinetic studies for nanomedicines.

Domaines: Maladies émergentes

Anne-Claire Groo, M Bossière, L Trichard, Pierre Legras, Jean-Pierre Benoît, et al.. In vivo evaluation of paclitaxel-loaded lipid nanocapsules after intravenous and oral administration on resistant tumor.. Nanomedicine, 2015, 10 (4), pp.589-601. ⟨10.2217/nnm.14.124⟩. ⟨hal-01153494⟩