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More than 50% of new drug candidates in drug discovery are lipophilic and exhibit poor aqueous solubility, which results in poor bioavailability and a lack of dose proportionality.Here, we improved the solubility of pedunculoside (PE) by generating a water-soluble inclusion complex composed of PE and the polymer β-cyclodextrin (CDP).We characterized this novel complex by 1H NMR, FT-IR, UV-vis spectroscopy, powder X-ray diffiactometry and thermogravimetric analysis.The ratio of β-cyclodextrin (β-CD) units in CDP to PE was determined to be 2 : 1.The KD value of the inclusion complex was determined to be 4.29×10-3 mol·L-1.In contrast to the low solubility of PE, the water-solubility of the PE-CDP complex was greatly enhanced.A preclinical toxicological study indicated that PE-CDP was well tolerated for a single administration.Importantly, the anti-inflammation potency of the PE-CDP complex was higher than that of PE.As a result, the formation of inclusion complexes by water-soluble CDP opens up possible aqueous applications of insoluble drug candidates in drug delivery.