High Drug Encapsulation Capacity in Cyclodextrin-Based Nanoparticles: Characterization and In Vivo Antitumor Efficacy in Tumor-Bearing Mice

Insufficient drug encapsulation, typically at about 10 wt %, remains a major challenge in the design of nanotechnology-based drug delivery systems. In this study, we created cyclodextrin-based nanoparticles (CDNP_PEGs), synthesized by the hyperbranched polymerization of cyclodextrins using a diepoxy poly(ethylene glycol) linker, which exhibited a high drug encapsulation capacity of up to 54 wt % using the xanthone derivative α-mangostin (MGS) as a model compound. Evaluation in a tumor-bearing mouse model indicated that a single intravenous administration via the tail vein induced a significantly greater antitumor effect compared with free MGS. These results demonstrate the potential of CDNP_PEGs as promising high-capacity carriers for the delivery of anticancer drugs.