ethosomes

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Liposomes- and Ethosomes-Associated Distamycins: a Comparative Study

Journal Title, Volume, Page: 
J Liposome Res. 2010 Dec;20(4):277-85. doi: 10.3109/08982100903443057. Epub 2009 Dec 4
Year of Publication: 
2009
Authors: 
Rita Cortesi
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Romeo Romagnoli
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Markus Drechsler
Macromolecular Chemistry II, University of Bayreuth, Germany
Enea Menegatti
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Abdel N. Zaid
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Laura Ravani
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Elisabetta Esposito
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Preferred Abstract (Original): 

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.

2384's picture

Liposomes- and Ethosomes-Associated Distamycins: A ‎Comparative Study

Authors: 
Zaid AN
College of Pharmacy, An-Najah National University, Nabul, Palestine.
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Cortesi R
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Romagnoli R
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Drechsler M
Macromolecular Chemistry II, University of Bayreuth, Germany
Menegatti E
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Esposito E
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Ravani L
Department of Pharmaceutical Sciences, University of Ferrara, Italy
Preferred Abstract (Original): 

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.

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