Transferrin/α-tocopherol modified poly(amidoamine) dendrimers for improved tumor targeting and anticancer activity of paclitaxel.

Aim: Transferrin anchored, poly(ethylene glycol) (PEG) and α-tocopheryl succinate (α-TOS) conjugated generation 4 dendrimer has been prepared in order to develop a tumor targeted delivery system of a hydrophobic chemotherapeutic agent, paclitaxel (PTX). Materials & methods: The dendrimers were characterized physicochemically for size, ζ and encapsulation ability. The cellular uptake, cytotoxicity potential and apoptosis of prepared nanoconstruct were evaluated in human cervical epithelial cells monolayer and 3D spheroids. Results & conclusion: G4-TOS-PEG-Tf demonstrated increased cellular uptake, cytotoxicity and apoptotic potential of PTX compared with free PTX and G4-TOS-PEG-PTX. G4-TOS-PEG-Tf-PTX inhibited growth of human cervical epithelial cells spheroids significantly. The newly developed dendrimers hold promise as an efficient delivery system for PTX or other hydrophobic chemotherapeutic agents for targeted delivery to tumors.