title: Liposomes- and ethosomes-associated distamycins: a comparative study.
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.
authors: Department of Pharmaceutical Sciences, University of Ferrara, Italy. crt@unife.it
authors: Rita
authors: R
authors: Cortesi
authors: Romeo
authors: R
authors: Romagnoli
authors: Markus
authors: M
authors: Drechsler
authors: Enea
authors: E
authors: Menegatti
authors: Abdel N
authors: AN
authors: Zaid
authors: Laura
authors: L
authors: Ravani
authors: Elisabetta
authors: E
authors: Esposito
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D001672:Biocompatible Materials / Q000737:chemistry / Q000378:metabolism; D002460:Cell Line; D004214:Distamycins / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism; D004355:Drug Stability; D000431:Ethanol / Q000737:chemistry*; D006801:Humans; D008081:Liposomes / Q000737:chemistry* / Q000378:metabolism* / Q000648:ultrastructure; D008422:Materials Testing; D051379:Mice; D015394:Molecular Structure; D010316:Particle Size; D013997:Time Factors
chemical_list: D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D004214:Distamycins; D004337:Drug Carriers; D008081:Liposomes; D000431:Ethanol