Ursolic acid is a pentacyclic triterpenoid carboxylic acid found in many plants and fruits like apples, basil and rosemary. The clinical efficacy of ursolic acid is limited due to its poor aqueous solubility. In present work inclusion complex of ursolic acid was prepared with water soluble polymeric derivative of B-CD (Epi-B-CD) using kneading method and characterized by FTIR and XRD. Phase solubility study was performed according to Higuchi's method and led to formation of A type solubility curve. The inclusion complex was prepared in 1:1 M ratio. There was linear increase in solubility with the increasing concentration of Epi-B-CD up to 20 mM. Ursolic acid is widely used in treatment of skin cancer. Nanolipid carriers were prepared by emulsification and lyophilisation method. The developed NLCS were characterized for particle size, zeta potential, entrapment efficiency (EE) and morphology. Studies were conducted to evaluate the effectiveness of the NLCS in improving the penetration rate. NLCS were found to have an average size of 103.4 2 0.3 nm, a zeta potential of -21.326.2 mV, and an EE of 69%. The anti-cancer activity was evaluated on animal model and in-vitro cell line studies. The results confirmed that cyclodextrin complexed ursolic acid was more potent as compared to pure drug. Also, there was reduction in dose with minimal side effects. Thus, complexation is a prominent tool for improving the biological activity of herbals.
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