Huan Wang,1,2,* Xiangui Li,1,* Zhiqiang Ma,1 Dan Wang,3 Linzhao Wang,1,2 Jieqiong Zhan,1,4 Lan She,1 Feng Yang1 1Department of Inorganic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, 2Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, 3Department of Obstetrics and Gynecology, Shanghai Changzheng Hospital, Second Military Medical University, Shanghai, 4Department of Pharmacy, Hebei North University, Zhangjiakou, Hebei, People's

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... ic of China *These authors contributed equally to this article Abstract: In this study, a highly effective transmembrane delivery vehicle based on PEGylated oxidized mesoporous carbon nanosphere (oMCN@PEG) was successfully fabricated in a facile strategy. oMCN@PEG exhibited a narrow size distribution of 90 nm, excellent hydrophilicity, good biocompatibility, and a very high loading efficiency for doxorubicin (DOX). The drug system (oMCN@DOX@PEG) exhibited excellent stability under neutral pH conditions, but with dramatic releases of DOX at reduced pH conditions. Pharmacokinetics study revealed that oMCN@DOX@PEG could prolong the circulation of DOX in the blood stream. The endocytosis, cytotoxicity, and anticancer effect in vitro and in vivo of the drug-loaded nanoparticles were also evaluated. Our results showed that the nanoparticles efficiently penetrated the membrane of tumor cells, subsequently released drugs, and efficiently inhibited the growth of cancer cells both in vitro and in vivo. Especially, oMCN@DOX@PEG also exhibited significant antimetastasis effect in advanced stage of malignant cancer, improving the survival time of tumor-bearing mice. The results suggested that oMCN@PEG might be a promising anticancer drug delivery vehicle for cancer therapy. Keywords: drug delivery, hydrophilic, mesoporous carbon nanoparticles, tumor metastasis