Tumor cell growth inhibition by liposome-encapsulated aromatic polyamidines.

Abstract

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.

• Authors: C Nastruzzi, R Gambari, E Menegatti, P Walde, P L Luisi
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 79 Issue 8 Pg. 672-7 (Aug 1990) ISSN: 0022-3549 [Print] United States
• PMID: 2231328 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Benzamidines
• Capsules
• Liposomes
• 4,4'-(2,2-bis((4-(aminoiminomethyl)-2-bromophenoxy)methyl)-1,3-propanediyl)bis(oxy))bis(3-bromobenzenecarboximidamide

Topics

• Antineoplastic Agents (administration & dosage, pharmacology)
• Benzamidines (administration & dosage, pharmacology)
• Breast Neoplasms (drug therapy)
• Capsules
• Chemistry, Pharmaceutical
• Freeze Fracturing
• Humans
• Kidney Neoplasms (drug therapy)
• Liposomes
• Melanoma (drug therapy)
• Permeability
• Spectrophotometry, Ultraviolet
• Tumor Cells, Cultured (drug effects)