Contact
    Start Publications Assessment of various formulation approaches for the ...
    ←  Publication Finder
    KSV NIMA

    Assessment of various formulation approaches for the application of beta-lapachone in prostate cancer therapy

    Year: 2020

    Journal: Int. J. Pharm., Volume 579, APR 15

    Authors: Wu, X; Kasselouri, A; Vergnaud-Gauduchon, J; Rosilio, V

    Organizations: China Scholarship Council (CSC)China Scholarship Council

    Keywords: Beta-lapachone; Double loaded liposome; Cyclodextrin; Poly-lactide; PC-3 cell; NQO1

    Beta-lapachone (beta-Lap) is an anticancer drug activated by the NAD(P)H:quinone oxidoreductase (NQO1), an enzyme over-expressed in a large variety of tumors. B-Lap is poorly soluble in water and in most biocompatible solvents. Micellar systems, liposomes and cyclodextrins (CDs) have been proposed for its solubilization. In this work, we analyzed the properties and in vitro efficacy of beta-Lap loaded in polymer nanoparticles, liposome bilayers, complexed with sulfobutyl-ether (SBE)- and hydroxypropyl (HP)-beta cyclodextrins, or double loaded in phospholipid vesicles. Nanoparticles led to the lowest drug loading. Encapsulation of [beta-Lap:CD] complexes in vesicles made it possible to slightly increase the encapsulation rate of the drug in liposomes, however at the cost of poor encapsulation efficiency. Cytotoxicity tests generally showed a higher sensitivity of NIH 3T3 and PNT2 cells to the treatment compared to PC-3 cells, but also a slight resistance at high beta-Lap concentrations. None of the studied beta-Lap delivery systems showed significant enhanced cytotoxicity against PC-3 cells compared to the free drug. Cyclodextrins and double loaded vesicles, however, appeared more efficient drug delivery systems than liposomes and nanoparticles, combining both good solubilizing and cytotoxic properties. Ligand-functionalized double loaded liposomes might allow overcoming the lack of selectivity of the drug.
    View publication