Rational Design of Intracellular Anticancer Drug Delivery: Nanocarriers Bearing Two-step Degradation Mechanism

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A glutathione-p-nitroaniline conjugate was synthesized and examined binding of the conjugate with glutathione S-transferase (GST). When the conjugate was titrated with GST, absorbance increased with increasing concentration of GST, suggesting the binding the conjugate with GST. In addition, p-nitroaniline release was observed in the presence of GST. As for the design of nanocarriers for the prodrug, polyglycerol dendrimers (PGDs) were subjected and examined to clarify their interaction with the anti-cancer drug, 5-fluorouracil (5-Fu). The results of 19F-, 1H-NMR and fluorescence spectroscopy to confirm that PGD could encapsulate 5-Fu under aqueous conditions. Another examination of nanocarrier preparations, a liposome consisting of PGD-based phospholipids and a polymeric micelle consisting of vitamin E and a biocompatible polymer.Through these studies, novel smart nanocarries in combination with the produg system toward GST targeting are feasible in near future.