Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Comparison of classical, stealth and super-stealth liposomes for intravenous delivery of lumefantrine: Formulation, characterization and pharmacodynamic study

Ebele Onuigbo¹ , Anthony Attama², Elena Canato³, Gianfranco Pasut³

¹Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka; ²Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Nigeria; ³Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua 35131, Italy.

For correspondence:- Ebele Onuigbo Email: ebele.onuigbo@unn.edu.ng Tel:+2348062995712

Accepted: 19 October 2020 Published: 30 November 2020

Citation: Onuigbo E, Attama A, Canato E, Pasut G. Comparison of classical, stealth and super-stealth liposomes for intravenous delivery of lumefantrine: Formulation, characterization and pharmacodynamic study. Trop J Pharm Res 2020; 19(11):2247-2253 doi: 10.4314/tjpr.v19i11.1

© 2020 The authors.
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Abstract

Purpose: To develop and compare classical liposomes (CL), stealth liposomes (SL) and super-stealth liposomes (SSL) encapsulating lumefantrine for intravenous administration.

Method: CL, SL or SSL were prepared by thin-layer evaporation method and evaluated for particle size, polydispersity index (PdI), encapsulation efficiency and short-term stability. Pharmacodynamic study using mice infected with Plasmodium berghei was also carried out.

Results: The particle sizes (nm) and PDI of the liposomes were: CL (248 ± 44.89; 0.78 ± 0.02), SL (235.8 ± 45.18; 0.39 ± 0.06) and SSL (238.2 ± 23.0; 0.24 ± 0.04). Encapsulation efficiency was highest in SSL (66 %), followed by SL (44.4 %) and then by CL (42.5 %). SSL was the most stable after 72 h of storage. In vivo, lumefantrine produced significant reduction in parasitaemia after 7 days (p < 0.05) by SSL (68.3 ± 8.9 %) followed by CL (55.8 ± 15.2 %) and then SL (53.4 ± 14.9 %).

Conclusion: SSL formulation of lumefantrine exhibits good physicochemical and pharmacodynamic potentials and should be further investigated in future studies for the treatment of malaria.

Keywords: Drug delivery, Classical liposomes, Stealth liposomes, Super-stealth liposomes, Lumefantrine, Malaria