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ORIGINAL RESEARCH ARTICLE
Year : 2017  |  Volume : 7  |  Issue : 4  |  Page : 155-163

Lipid nanocapsules formulation and cellular activities evaluation of a promising anticancer agent: EAPB0503


1 CNRS, ENSCM, IBMM, University of Montpellier, Montpellier, France
2 UMR 5253, CNRS, ENSCM, University of Montpellier, Institut Charles Gerhardt Montpellier, Montpellier, France

Correspondence Address:
Prof. Carine Deleuze-Masquefa
UFR Pharmacie, 15 Avenue Charles Flahault, 34 000 Montpellier
France
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/jphi.JPHI_53_17

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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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