Cidofovir (HPMPC) was recently reported to exert a valuable antineoplastic activity against primary effusion lymphoma (PEL), a B-cell neoplasm associated with Human Herpesvirus-8 (HHV-8) infection. In this study, we developed and characterized liposomes encapsulating HPMPC to increase drug efficacy reducing the administered dose and the related toxicity, which actually hamper its clinical therapeutic use in patients affected with PEL. The liposomes, obtained using different formulations of neutral and cationic lipids, were analyzed by microscopical (AFM) and spectroscopical (PCS and NMR) techniques. Using an in vitro model of PEL (BCBL-1 cell line), the carrier toxicity and the antineoplastic efficacy of liposomes were evaluated by flow cytometry applying apoptosis and cell death analysis. The in vitro study showed the applicability of the liposomes within a restricted range of lipidic concentrations according to the lipids used during the preparation. The moderate increases in the percentage of apoptotic/necrotic cells suggests that liposomal delivery allows the release of HPMPC into BCBL-1 cells enabling an unexpectedantineoplastic activity of this drug even at lower doses.
Cidofovir-loaded liposomes: an intro-study using BCBL-1 cell line as a model for primary effusion lymphoma / Ruozi, Barbara; Riva, Giovanni; Belletti, Daniela; Tosi, Giovanni; Forni, Flavio; Mucci, Adele; Barozzi, Patrizia; Luppi, Mario; Vandelli, Maria Angela. - In: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0928-0987. - STAMPA. - 41:2(2010), pp. 254-264. [10.1016/j.ejps.2010.06.012]
Cidofovir-loaded liposomes: an intro-study using BCBL-1 cell line as a model for primary effusion lymphoma
RUOZI, Barbara;RIVA, Giovanni;BELLETTI, Daniela;TOSI, Giovanni;FORNI, Flavio;MUCCI, Adele;BAROZZI, Patrizia;LUPPI, Mario;VANDELLI, Maria Angela
2010
Abstract
Cidofovir (HPMPC) was recently reported to exert a valuable antineoplastic activity against primary effusion lymphoma (PEL), a B-cell neoplasm associated with Human Herpesvirus-8 (HHV-8) infection. In this study, we developed and characterized liposomes encapsulating HPMPC to increase drug efficacy reducing the administered dose and the related toxicity, which actually hamper its clinical therapeutic use in patients affected with PEL. The liposomes, obtained using different formulations of neutral and cationic lipids, were analyzed by microscopical (AFM) and spectroscopical (PCS and NMR) techniques. Using an in vitro model of PEL (BCBL-1 cell line), the carrier toxicity and the antineoplastic efficacy of liposomes were evaluated by flow cytometry applying apoptosis and cell death analysis. The in vitro study showed the applicability of the liposomes within a restricted range of lipidic concentrations according to the lipids used during the preparation. The moderate increases in the percentage of apoptotic/necrotic cells suggests that liposomal delivery allows the release of HPMPC into BCBL-1 cells enabling an unexpectedantineoplastic activity of this drug even at lower doses.File | Dimensione | Formato | |
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