Employing rubusoside to improve the solubility and permeability of antitumor compound betulonic acid

Aim: To examine if rubusoside (RUB) can overcome insolubility of betulonic acid (BEA), it can be accurately evaluated for its intrinsic activity against cancer in cell culture and in tumor animal models. Materials & methods: By processing RUB and BEA together using a solvent evaporation method, a joint nanoparticulate structure is formed, designated as BEA-NP. Results: BEA-NP was found over three-times more permeable than that solubilized by DMSO in Caco-2 cell monocultures. In an in vivo efficacy study, the tumor growth in the S180 berry mice orally dosed with BEA-NP at 75 mg/kg was inhibited by 50%. Conclusion: RUB was effective in solubilizing BEA, maintaining its cytotoxicity, enhancing its permeability and reducing tumor growth when orally administered.