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Berberine, a widely used isoquinoline alkaloid in traditional Chinese medicine, has been proved to be a potential candidate in liver cancer therapy. However, the low therapeutic dose in the tumor target which is due to the poor solubility and oral bioavailability has limited its clinical application. In this study, fluorescent selfcarried Berberine microrods (Ber-MRs) were prepared in gram-scale through a facile and cheap antisolvent precipitation method. Ber-MRs exhibited good optical properties, pH-responsive drug release behavior and selective and safe antitumor performance in vitro and in vivo without obvious toxicity. These findings have demonstrated that Ber-MRs are promising for efficient and safe liver cancer therapy.These authors contributed equally to this work.