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Eur J Pharm Biopharm. 2012 Aug;81(3):690-3. doi: 10.1016/j.ejpb.2012.04.012. Epub 2012 Apr 26.

Brain tumour targeting strategies via coated ferrociphenol lipid nanocapsules.

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Ingénierie de lVectorisation Particulaire in Micro et Nanomédecines Biomimétiques, LUNAM Université, Angers, France.


In this study, a new active targeting strategy to favour ferrociphenol (FcdiOH) internalisation into brain tumour cells was developed by the use of lipid nanocapsules (LNCs) coated with a cell-internalising peptide (NFL-TBS.40-63 peptide) that interacts with tubulin-binding sites. In comparison, OX26 murine monoclonal antibodies (OX26-MAb) targeting transferrin receptors were also inserted onto the LNC surface. The incorporation of OX26 or peptide did not influence the in vitro antiproliferative effect of FcdiOH-LNCs on the 9L cells since their IC50 values were found in the same range. In vivo, intracerebral administration of OX26-FcdiOH-LNCs or peptide-FcdiOH-LNCs by convection enhanced delivery did not enhance the animal median survival time in comparison with untreated rats (25 days). Interestingly, intra-carotid treatment with peptide-FcdiOH-LNCs led to an ameliorated survival time of treated rats with the presence of animals surviving until days 35, 40 and 44. Such results were not obtained with OX26-MAbs, demonstrating the benefit of NFL-TBS.40-63 peptide as an active ligand for peripheral drug delivery to the brain tumours.

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