title: Employing rubusoside to improve the solubility and permeability of antitumor compound betulonic acid.
abstract: OBJECTIVE
  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.
  
  
  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%.
  
  
  CONCLUSIONS
  RUB was effective in solubilizing BEA, maintaining its cytotoxicity, enhancing its permeability and reducing tumor growth when orally administered.
authors.affiliation: Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, People's Republic of China.|School of Perfume & Aroma Technology, Shanghai Institute of Technology, Shanghai 201418, People's Republic of China.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, People's Republic of China.
authors.forename: Guixin
authors.initials: G
authors.lastname: Chou
authors.affiliation: School of Renewable Natural Resources, Louisiana State University Agricultural Center, Baton Rouge, LA 70803, USA.
authors.forename: Zhijun
authors.initials: Z
authors.lastname: Liu
authors.affiliation: School of Renewable Natural Resources, Louisiana State University Agricultural Center, Baton Rouge, LA 70803, USA.
authors.forename: Mei
authors.initials: M
authors.lastname: Liu
keywords: betulonic acid; cytotoxicity; nanoparticle; permeability enhancement; solubilization; tumor mice