Title: Preparation of liposomes containing benzophenanthridine alkaloid sanguinarine and evaluation of its cytotoxic activity

Authors: N.B. Feldman; V.N. Kuryakov; N.E. Sedyakina; T.I. Gromovykh; S.V. Lutsenko

Addresses: Department of Biotechnology, Federal State Autonomous Educational Institution of Higher Education I.M. Sechenov First Moscow State Medical University of the Ministry of Health of the Russian Federation (Sechenov University), 2-4 Bolshaya Pirogovskaya St., 119991 Moscow, Russia ' E.E. Gorodetsky Phase Transition and Critical Phenomena Laboratory, Oil and Gas Research Institute of the Russian Academy of Sciences, Gubkina St., 119333 Moscow, Russia ' Department of Biotechnology, Federal State Autonomous Educational Institution of Higher Education I.M. Sechenov First Moscow State Medical University of the Ministry of Health of the Russian Federation (Sechenov University), 2-4 Bolshaya Pirogovskaya St., 119991 Moscow, Russia ' Department of Biotechnology, Federal State Autonomous Educational Institution of Higher Education I.M. Sechenov First Moscow State Medical University of the Ministry of Health of the Russian Federation (Sechenov University), 2-4 Bolshaya Pirogovskaya St., 119991 Moscow, Russia ' Department of Biotechnology, Federal State Autonomous Educational Institution of Higher Education I.M. Sechenov First Moscow State Medical University of the Ministry of Health of the Russian Federation (Sechenov University), 2-4 Bolshaya Pirogovskaya St., 119991 Moscow, Russia

Abstract: Sanguinarine is a plant alkaloid with relatively low toxicity and high antiangiogenic, antitumour and antiviral potential. In order to increase its bioavailability and effectiveness, sanguinarine liposomes were prepared by a reverse phase evaporation method and characterised. Dynamic light scattering showed mean liposome size of 65 ± 11 nm, zeta-potential equal to -54 ± 1.2 mV, and polydispersity index equal to 0.26. The encapsulation efficiency was 78.6 ± 5.1%. The study on experimental models showed a prolonged sanguinarine release from liposome preparations. Liposomal sanguinarine showed dose-dependent cytotoxic activity in vitro on B16 (murine melanoma) and HeLa (human cervical carcinoma) cell lines. The highest cytotoxicity was observed on B16 cell line (IC50 6.5 μM). HeLa cell line cytotoxicity was relatively lower, equal to 8.03 μМ. Compared with free sanguinarine, liposomal sanguinarine may have advantages for in vivo anticancer therapy, due to its lower toxicity and 'passive targeting' as a result of enhanced permeability of tumour vessels.

Keywords: sanguinarine; liposomes; bioavailability; drug release; cytotoxic activity.

DOI: 10.1504/IJNT.2018.094785

International Journal of Nanotechnology, 2018 Vol.15 No.4/5, pp.280 - 287

Available online: 10 Sep 2018 *

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