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Dose effect activity of ferrocifen-loaded lipid nanocapsules on a 9L-glioma model

Abstract : Ferrociphenol (Fc-diOH) is a new molecule belonging to the fast-growing family of organometallic anticancer drugs. In a previous study, we showed promising in vivo results obtained after the intratumoural subcutaneous administration of the new drug-carrier system Fc-diOH-LNCs on a 9L-glioma model. To further increase the dose of this lipophilic entity. we have created a series of prodrugs of Fc-diOH. The phenol groups were protected by either an acetyl (Fc-diAc) or by the long fatty-acid chain of a palmitate (Fc-diPal). LNCs loaded with Fc-diOH prodrugs have to be activated in situ by enzymatic hydrolysis. We show here that the protection of diphenol groups with palmitoyl results in the loss of Fc-diOH in vitro activity, probably due to a lack of in situ hydrolysis. On the contrary, protection with an acetate group does not affect the strong, in vitro, anti proliferative effect of ferrocifen-loaded-LNCs neither the reduction of tumour volume observed on an ectopic model, confirming that acetate is easily cleaved by cell hydrolases. Moreover, the cytostatic activity of Fc-diOH-LNCs is confirmed on an orthotopic glioma model since the difference in survival time between the infusion of 0.36 mg/rat Fc-diOH-LNCs and blank LNCs is statistically significant. By using LNCs or Labrafac (R) to carry the drug, a dose-effect ranging from 0.005 to 2.5 mg of Fc-diOH per animal can be evidenced. (C) 2009 Elsevier B.V. All rights reserved.
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E. Allard, N. T. Huynh, A. Vessières, Pascal Pigeon, G. Jaouen, et al.. Dose effect activity of ferrocifen-loaded lipid nanocapsules on a 9L-glioma model. International Journal of Pharmaceutics, Elsevier, 2009, 379 (2), pp.317-323. ⟨10.1016/j.ijpharm.2009.05.031⟩. ⟨hal-01230396⟩



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