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Research Article

Liposomes- and ethosomes-associated distamycins: a comparative study

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Pages 277-285 | Received 22 Jun 2009, Accepted 27 Oct 2009, Published online: 04 Dec 2009
 

Abstract

The present article describes a comparative study of the performances of liposomes and ethosomes as specialized delivery systems for distamycin A (DA) and two of its derivatives. Liposomes and ethosomes were prepared by classical methods, extruded through polycarbonate filters, and characterized in terms of dimensions, morphology, and encapsulation efficiency. It was found that DA was associated with vesicles (either liposomes or ethosomes) by around 16.0%, while both derivatives of DA showed a percentage of association around 80% in the case of liposomes and around 50% in the case of ethosomes. In vitro antiproliferative activity experiments performed on cultured human and mouse leukemic cells demonstrated that vesicles were able to increase the activity of both derivatives of DA. In addition, it was demonstrated that the aging of both liposomes- and ethosomes-associated distamycin suspensions did not heavily influence the vesicle size, while all samples showed a relevant drug leakage with time. Moreover, according to the different physicochemical characteristics of DA and its derivatives (i.e., log P), vesicle-associated DA showed the highest loss of drug with respect to both its derivatives. In conclusion, the enhancement of drug activity expressed by these specialized delivery systems-associated DD could be interesting to obtain an efficient therapeutic effect aimed at reducing or minimizing toxic effects occurring with distamycins administration.

Acknowledgements

The authors are grateful to Dr. Elena Esposito (MSc Conference Interpreter and Translator) and Prof. Raffaella Ocone (MEng, PhD, FRSE) for their linguistic revision of the manuscript for this article.

Declaration of interest

The authors thank the “Ministry of Education, University and Research of Italy” (MIUR) and “Fondazione Cassa di Risparmio di Cento” for their financial support.

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