Abstract

It is new approach to combine one or multiple drugs onto the same drug-delivery nanocarrier in accurately controllable manner, by covalently preconjugating one or multiple therapeutic agents by covalent bond to form drug conjugates. It provides the advantages of nano size system with the targeted delivery of drug with great precision. The conjugation system allows the modification in the metabolic path way in the blood stream and can target the delivery to the heart, liver or brain. The cleavable covalent bond allows the therapeutic activity of the individual drugs to be resumed after the drug conjugates are delivered into the target site and get separated from the carriers. The characters of drug conjugated system are (a) a covalent bond between drug and carrier moiety, (b) in vitro cleavage of the bond, (c) optimum release of drug at site of action to ensure effectiveness, (d) no alteration in drug action. As a proof of the concept, synthesis and characterization of stearic acid/oleic acid- diminazene conjugates nanoparticles are demonstrated. It is shown that after conjugation with lipid and/or polymer and synthesized to nanoparticles there is significant improvement in cyctotoxicity and targeted controlled delivery of drug than the free drug.

Keywords: Carriers, Lipid-drug conjugation, Metabolism, Modification, Nanomedicine, Polymer-drug conjugation.