PAMAM dendrimer-platinum conjugates

PAMAM Dendrimer-Platinum Conjugates and Applications 2.1 PAMAM Dendrimer-Encapsulated Platinum Nanoparticles... 

Duncan and co-workers also created one of the first covalently linked DDS based on a dendrimer scaffold [52]. Carboxylated (COOH) PAMAM dendrimers were used to attach cisplatin, a common chemotherapeutic in clinical use. The covalent attachment of the drug increases the specific solubility of cisplatin ten-fold, and enables a loading of approximately 25% to be achieved for the PAMAM dendrimer. However, dendrimer clusters form as a consequence of the multiple COOH groups on the dendrimer scaffold and intermolecular reactions involving cisplatin. In vitro evaluation has shown that the covalent conjugation to the dendrimer results in a lower toxicity, and in vivo experiments have shown that the blood clearance rate is lower, with higher intra-tumoral concentrations of platinum than those achieved with the free drug. 

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