Betulinic Acid in Complex with a Gamma-Cyclodextrin Derivative Decreases Proliferation and in Vivo Tumor Development of Non-Metastatic and Metastatic B164A5 Cells

• Main Authors: Codruta Soica, Corina Danciu, Germaine Savoiu-Balint, Florin Borcan, Rita Ambrus, Istvan Zupko, Florina Bojin, Dorina Coricovac, Sorina Ciurlea, Stefana Avram, Cristina Adriana Dehelean, Teodora Olariu, Petru Matusz
• Format: Article
• Language: English
• Published: MDPI AG 2014-05-01
• Series: International Journal of Molecular Sciences
• Subjects: betulinic acid; DSC; X-ray diffraction; SEM; MTT test; C57BL/6J mice
• Online Access: http://www.mdpi.com/1422-0067/15/5/8235

Betulinic acid, a very promising anti-melanoma agent, has very low water solubility that causes low bioavailability. To overcome this inconvenience, a highly water-soluble cyclodextrin was used (octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonic acid)]-γ-cyclodextrin). The complex was physico-chemically analyzed using differential scanning calorimetry (DSC), X-ray and scanning electron microscopy (SEM) methods and then in vitro tested for its antiproliferative activity by the MTT assay and by cell cycle analysis. Finally, the complex was tested in vivo using an animal model of murine melanoma developed in C57BL/6J mice, where it caused a reduction in tumor volume and weight. The study revealed the beneficial influence of betulinic acid inclusion into the cyclodextrin in terms of antiproliferative activity and in vivo tumor development.