A newly synthesized polyhydroxy aromatic compound(LG 106W) has good skin lightening effect. Inclusion complexation of LG 106W with β -cyclodextrin and its hydroxypropyl and dimethyl derivatives was studied by the solubility method, scanning electron microscopy and differential thermal analysis. A relationship between host and guest was clearly reflected in the magnitude of the stability constant(DM- β > HP- β >β -cyclodextrin). Formulation problems, which resulted from its very low solubility in aqueous solution, were resolved by the inclusion formation. LG 106W from inclusions is much more water-soluble than pure one. The improvement of pH and temperature stability correlated with the increased solubility was also observed. Inclusion complex of LG 106W had similar activity to pure LG 106W on the inhibition of melanin synthesis in B-16 melanoma cell but showed lower irritation on cultured cell test in vitro. According to the results, cyclodextrins might be one of the reliable candidates for improving the availability of LG 106W.