ABSTRACT

In 1975, Helmut Ringsdorf presented his idea regarding the use of polymers as targetable drug carriers [1]. He foresaw the basic

Hemda Baabur-Cohen,* Liora Omer,* and Ronit Satchi-Fainaro Department of Physiology and Pharmacology, Sackler School of Medicine, Tel Aviv University, Tel Aviv 69978, Israel ronitsf@post.tau.ac.il

Handbook of Harnessing Biomaterials in Nanomedicine: Preparation, Toxicity, and Applications Edited by Dan Peer Copyright © 2012 Pan Stanford Publishing Pte. Ltd. ISBN 978-981-4316-46-0 (Hardback), 978-981-4364-27-0 (eBook) www.panstanford.com

architecture of polymer-drug conjugates: a polymeric spacer, drug attached via a hydrolytically or enzymatically cleavable spacer and a targeting group complementary to a receptor/antigen at the target cell. Since then, most of the polymer-drug conjugates have been designed and developed according to Ringsdorf’s model (Figure 4.1A). Most of the earlier systems rarely advanced beyond in vitro testing. However, over the last 15 years, a growing number of polymer therapeutics have been synthesized and characterized. In particular, PEG-protein conjugates have reached the market, and polymer-drug conjugates and polymeric micelles entered clinical trials mainly as anti-cancer agents.