Liposomes and micellar dispersions for delivery of benzoheterocyclic derivatives of distamycin A.
In this article we describe the production and characterization of specialized delivery systems for some distamycin derivatives (DD), namely liposomes and micellar dispersions. All the formulations were designed to increase the solubility of DD in an aqueous environment and to reduce the possible toxicity problems related to the administration of these drugs. For instance, liposomes were prepared by reverse phase evaporation technique followed by extrusion through polycarbonate filters, then characterized in terms of dimensions, morphology, and encapsulation efficacy. The analysis of their in vitro antiproliferative activity on cultured human and mouse leukemic cells demonstrated that liposomes and micellar dispersions containing DD exert quite different effects. These effects were compared with those shown by the free drug depending on type of drug and also cell line used.
Cortesi
R
R
Department of Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy. crt@unife.it
Esposito
E
E
Cuccu
I
I
Romagnoli
R
R
Menegatti
E
E
Zaid
A N
AN
Nastruzzi
C
C
D000818:Animals; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D004214:Distamycins / Q000008:administration & dosage* / Q000494:pharmacology*; D004337:Drug Carriers; D016503:Drug Delivery Systems; D004355:Drug Stability; D005614:Freeze Fracturing; D006571:Heterocyclic Compounds / Q000008:administration & dosage* / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells; D007939:Leukemia L1210 / Q000188:drug therapy; D008081:Liposomes; D008567:Membranes, Artificial; D051379:Mice; D008823:Micelles; D008854:Microscopy, Electron; D010316:Particle Size; D012995:Solubility
D004214:Distamycins; D004337:Drug Carriers; D006571:Heterocyclic Compounds; D008081:Liposomes; D008567:Membranes, Artificial; D008823:Micelles; C030000:stallimycin