We demonstrated a new concept employing the drug molecules themselves as components of nanocarriers to substantially increase the drug loading content, minimize the use of inactive materials, and suppress the premature drug burst release. Taking advantage of the hydrophobicity of CPT, two CPT molecules were conjugated to a short PEG chain, forming an amphiphilic phospholipid-like molecule, PEG-DiCPT. PEG-DiCPT formed stable liposome-like nanocapsules with a CPT loading content as high as 58 wt% without burst release in aqueous solution. PEG-DiCPT itself was a prodrug releasing CPT once inside cells, which showed high in vitro and in vivo antitumor activity. Meanwhile, the formed nanocapsules could be loaded with a water-soluble drug such as DOX�HCl with high loading efficiency. The DOX�HCl�loaded nanocapsules delivered two anticancer drugs producing a synergetic cytotoxicity to cancer cells. This prodrug nanocapsule is a new efficient drug carrier for cancer chemotherapy.

Prodrug lipid forming high drug loading multifunctional nanocapsules

239th National Meeting (2010)

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