ANTIPROLIFERATIVE ACTIVITY OF β-LAPACHONE-LOADED LIPOSOMES AGAINST HUMAN PROSTATE CARCINOMA CELLS

Autoria: Isabella Macário Ferro Cavalcanti; Bárbara Teixeira Belo; Beatriz Oliveira Barros; Zion Nascimento de Souza; Mariane Cajubá de Britto Lira Nogueira; Ana Carolina Pavanelli; Luís André de Almeida Campos; Maria Aparecida Nagai; Nereide Stela Santos Magalhães

Coletânea: Pesquisas em Temas de Ciências da Saúde

DOI: 10.46898/rfb.mrwgmcy7cgba

Resumo

The aim of this study was to evaluate the in vitro activity of conventional and stealth liposomes encapsulating β-lap or β-lap:HPβ-CD inclusion complex against human prostate carcinoma cells (DU-145). Liposomes were prepared by lipid film hydration, and the cytotoxicity was determined by MTT assay. The β-lap or β-lap:HPβ-CD encapsulated into liposomes presented equal or slightly higher IC70 when compared to the free molecule (2.5 μM), evidencing that β-lap was so active that the liposomes were 1.3 to 1.8-fold more active than the systems developed. The confocal microscopy revealed that the DU-145 cells presented the first evidence of a decrease in their viability and morphological alterations, such as mitotic figures, condensation of chromatin, nucleus fragmentation, apoptotic bodies, and giant cells with the increase of the β-lap concentration in solution or encapsulated into liposomes. The cell line DU-145 appears to have low internalization efficiency for both conventional and stealth liposomes; therefore, our formulations showed activity equal to or slightly lower than that of the free drug. In that way, the encapsulation of β-lap or β-lap:HPβ-CD into conventional or stealth liposomes described in this work could optimize the therapeutic application of this promising drug. Furthermore, this study encourages future research on the pharmacokinetics, biodistribution, and in vivo antitumor activity of the developed liposomes.

Palavras-chave: β-lapachone, 2-hydroxypropyl-β-cyclodextrin, liposomes, cytotoxicity, DU-145 cells