Apart from its antiproteinase activity, the aromatic polyamidine TAPP‐Br [the bromo derivative of 1, 3‐di‐(p‐amidinophenoxy)‐2, 2‐bis‐(p‐amidinophenoxymethy l)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. Copyright © 1990 Wiley‐Liss, Inc., A Wiley Company
Tumor cell growth inhibition by liposome‐encapsulated aromatic polyamidines
NASTRUZZI, Claudio;GAMBARI, Roberto;
1990
Abstract
Apart from its antiproteinase activity, the aromatic polyamidine TAPP‐Br [the bromo derivative of 1, 3‐di‐(p‐amidinophenoxy)‐2, 2‐bis‐(p‐amidinophenoxymethy l)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. Copyright © 1990 Wiley‐Liss, Inc., A Wiley CompanyI documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
