Users Online: 585 | Home Print this page Email this page
Home About us Editorial board Search Ahead of print Current issue Archives Submit article Instructions Subscribe Contacts Login 
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
Login to access the Email id

Source of Support: None, Conflict of Interest: None

DOI: 10.4103/jphi.JPHI_53_17

Rights and Permissions

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.

Print this article     Email this article
 Next article
 Previous article
 Table of Contents

 Similar in PUBMED
   Search Pubmed for
   Search in Google Scholar for
 Related articles
 Citation Manager
 Access Statistics
 Reader Comments
 Email Alert *
 Add to My List *
 * Requires registration (Free)

 Article Access Statistics
    PDF Downloaded250    
    Comments [Add]    

Recommend this journal