Macromolecular and nanotechnological modification of camptothecin and its analogs to improve the efficacy.
Camptothecin (CPT) and its analogs are some of the most potent antitumor agents known. However, their poor water-solubility and high toxicity require changes of their physicochemical and biological characteristics. Active lactone forms have provoked interest in the utility of CPT and its analogs again. Macromolecular chemical modifications and nanotechnological formulations have been used to obtain improved systems of CPT-related compounds. In these systems, one of the most important concepts is the enhanced permeability and retention (EPR) effect. The outcomes obtained by these approaches are displayed by introducing concrete examples.
Onishi
Hiraku
H
Department of Drug Delivery Research, Hoshi University, 2-4-41, Ebara, Tokyo 142-8501, Japan. onsihi@hoshi.ac.jp
Machida
Yoshiharu
Y
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D002166:Camptothecin / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D003911:Dextrans / Q000737:chemistry / Q000493:pharmacokinetics; D019073:HT29 Cells; D006801:Humans; D008081:Liposomes; D049329:Nanostructures; D009368:Neoplasm Transplantation; D011108:Polymers / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry; D011355:Prodrugs; D019772:Topotecan / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D016896:Treatment Outcome
D000972:Antineoplastic Agents, Phytogenic; D003911:Dextrans; D008081:Liposomes; D011108:Polymers; D011109:Polymethacrylic Acids; D011355:Prodrugs; C410030:T 2153; C011533:Duxon; D019772:Topotecan; C014392:carboxymethyl dextran; C410031:T 0128; D002166:Camptothecin