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Introduction: Oxymatrine (OM) is a kind of alkaloid extracted from a Chinese herb, which has been found to possess anti-hepatic fibrosis effect, but its anti-fibrotic potential may be limited due to poor distribution in liver and a risk of adverse effects.In this study, we developed a novel targeted drug delivery system based on OM-loaded polymersomes (PM) modified with the peptide RGD (RGD-PM-OM).Then, tissue biodistribution behavior was investigated in mice by a developed a rapid, high selective UPLC-ESI-MS/MS method.