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In antitumor efficacy in vivo, Tf/SA-R6H4-TBG-MEs exhibited the strongest inhibition of tumor growth and the longest survival period among all the groups, which is associated with the rational combination, microemulsion system, and dual modification with tumor-targeted ligands. Importantly, Tf/SA-R6H4-TBG-MEs significantly reduced the toxicity of tripterine against the liver and kidney. Our design provides a new approach for efficient and safe ovarian cancer therapy based on a multicomponent combination.This paper considers multiple imputation (MI) approach