Lipid Nanocapsules Formulation and Cellular Activities Evaluation of a Promising Anticancer Agent: EAPB0503

  • Adrien Chouchou CNRS, ENSCM, IBMM, University of Montpellier, Montpellier, France
  • Anne Aubert-Pouëssel UMR 5253, CNRS, ENSCM, University of Montpellier, Institut Charles Gerhardt Montpellier, Montpellier, France
  • Christophe Dorandeu UMR 5253, CNRS, ENSCM, University of Montpellier, Institut Charles Gerhardt Montpellier, Montpellier, France
  • Zahraa Zghaib CNRS, ENSCM, IBMM, University of Montpellier, Montpellier, France
  • Pierre Cuq CNRS, ENSCM, IBMM, University of Montpellier, Montpellier, France
  • Jean-Marie Devoisselle UMR 5253, CNRS, ENSCM, University of Montpellier, Institut Charles Gerhardt Montpellier, Montpellier, France
  • Pierre-Antoine Bonnet CNRS, ENSCM, IBMM, University of Montpellier, Montpellier, France
  • Sylvie Bégu UMR 5253, CNRS, ENSCM, University of Montpellier, Institut Charles Gerhardt Montpellier, Montpellier, France
  • Carine Deleuze-Masquefa CNRS, ENSCM, IBMM, University of Montpellier, Montpellier, France
Keywords: Cancer chemotherapy, Encapsulation, Formulation, Imiqualines, Nanocapsules, Solubility

Abstract

Objective: EAPB0503, lead compound of imiqualines, presented high antitumor activities but also a very low water solubility which was critical for further preclinical studies. To apply to EAPB0503, a robust and safe lipid formulation already used for poor soluble anticancer agents for injectable administration at a concentration higher than 1 mg/mL. Materials and Methods: Physicochemical properties of EAPB0503 were determined to consider an adapted formulation. In a second time, lipid nanocapsules (LNC) formulations based on the phase-inversion process were developed for EAPB0503 encapsulation. Then, EAPB0503 loaded-LNC were tested in vitro on different cell lines and compared to standard EAPB0503 solutions. Results: Optimized EAPB0503 LNC displayed an average size of 111.7 ± 0.9 nm and a low polydispersity index of 0.059 ± 0.002. The obtained loading efficiency was higher than 96% with a drug loading of 1.7 mg/mL. A stability study showed stability during 4 weeks stored at 25°C. In vitro results highlighted similar efficiencies between LNC and standard EAPB0503 solutions prepared in dimethyl sulfoxide. Conclusion: In view of results obtained for loading efficiency and drug loading, the use of a LNC formulation is very interesting to permit the solubilization of a lipophilic drug and to improve its bioavailability. Preliminary tested pharmaceutical formulation applied to EAPB0503 significantly improved its water solubility and will be soon considered for future preclinical in vivo studies.

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Chemical structures of imiqualines lead compounds: (a) EAPB0203 and (b) EAPB0503
Published
2018-04-06
How to Cite
1.
Chouchou A, Aubert-Pouëssel A, Dorandeu C, Zghaib Z, Cuq P, Devoisselle J-M, Bonnet P-A, Bégu S, Deleuze-Masquefa C. Lipid Nanocapsules Formulation and Cellular Activities Evaluation of a Promising Anticancer Agent: EAPB0503. ijpi [Internet]. 6Apr.2018 [cited 31Jul.2021];7(4):155-63. Available from: https://www.jpionline.org/index.php/ijpi/article/view/230