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Results The obtained data indicated that the prepared CPT-loaded lipopolymersome at a PEG-PLA DPPC ratio of 7525 exhibited superior stability and high loading capacity compared to other systems. Moreover, high cytotoxicity of the aptamer-targeted lipopolymersome and increased tumor accumulation were observed in comparison with non-targeted one.Conclusions The designed polymer-rich lipopolymersomal platform offers bright future for the development of potent nanomedicine against cancer.A new benzofuran derivative, nervione (1), was isolated