Tumor cell growth inhibition by liposome-encapsulated aromatic polyamidines.
Apart from its antiproteinase activity, the aromatic polyamidine TAPP-Br [the bromo derivative of 1,3-di-(p-amidinophenoxy)-2,2-bis-(p-amidinophenoxymethyl)propane (TAPP-H)] is able to inhibit the in vitro growth of a variety of tumor cell lines, including human melanoma, and breast and kidney carcinoma. We have now shown that TAPP-Br can efficiently be encapsulated into egg phosphatidylcholine vesicles. When incorporated into these liposomes, the inhibitory effect of TAPP-Br is significantly enhanced compared with that of the free drug. Based on these promising results, a proposal is made for the delivery of this antiproliferative agent to tumor cells by using liposomes as the vehicle.
Nastruzzi
C
C
Institut für Polymere, ETH-Zentrum, Zürich, Switzerland.
Gambari
R
R
Menegatti
E
E
Walde
P
P
Luisi
P L
PL
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001550:Benzamidines / Q000008:administration & dosage* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D005614:Freeze Fracturing; D006801:Humans; D007680:Kidney Neoplasms / Q000188:drug therapy; D008081:Liposomes; D008545:Melanoma / Q000188:drug therapy; D010539:Permeability; D013056:Spectrophotometry, Ultraviolet; D014407:Tumor Cells, Cultured / Q000187:drug effects*
D000970:Antineoplastic Agents; D001550:Benzamidines; D002214:Capsules; D008081:Liposomes; C057886:4,4'-(2,2-bis((4-(aminoiminomethyl)-2-bromophenoxy)methyl)-1,3-propanediyl)bis(oxy))bis(3-bromobenzenecarboximidamide