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Lauroyl-gemcitabine-loaded lipid nanocapsule hydrogel for the treatment of glioblastoma

Abstract :

The local delivery of chemotherapeutic agents is a very promising strategy for the treatment of glioblastoma (GBM). Gemcitabine is a chemotherapeutic agent that has a different mechanism of action compared to alkylating agents and shows excellent radio-sensitizing properties. So, we developed an injectable gel-like nanodelivery system consisting in lipid nanocapsules loaded with anticancer prodrug lauroyl-gemcitabine (GemC12-LNC) in order to obtain a sustained and local delivery of this drug in the brain. In this study, the GemC12-LNC has been formulated and characterized and the viscoelastic properties of the hydrogel were evaluated after extrusion from 30G needles. This system showed a sustained and prolonged in vitro release of the drug over one month. GemC12 and the GemC12-LNC have shown increased in vitro cytotoxic activity on U-87 MG glioma cells compared to the parent hydrophilic drug. The GemC12-LNC hydrogel reduced significantly the size of a subcutaneous human GBM tumor model compared to the drug and short-term tolerability studies showed that this system is suitable for local treatment in the brain. In conclusion, this proof-of-concept study demonstrated the feasibility, safety and efficiency of the injectable GemC12-LNC hydrogel for the local treatment of GBM.

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Journal articles
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https://hal.archives-ouvertes.fr/hal-01388804
Contributor : Okina Université d'Angers <>
Submitted on : Thursday, October 27, 2016 - 3:25:00 PM
Last modification on : Sunday, May 24, 2020 - 2:18:04 AM

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C Bastiancich, K Vanvarenberg, B Ucakar, Marion Pitorre, Guillaume Bastiat, et al.. Lauroyl-gemcitabine-loaded lipid nanocapsule hydrogel for the treatment of glioblastoma. Journal of Controlled Release, Elsevier, 2016, 225, pp.283-293. ⟨10.1016/j.jconrel.2016.01.054⟩. ⟨hal-01388804⟩

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