Abstract |
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.
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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 |
Journal | International journal of molecular sciences
(Int J Mol Sci)
Vol. 15
Issue 5
Pg. 8235-55
(May 09 2014)
ISSN: 1422-0067 [Electronic] Switzerland |
PMID | 24821543
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Drug Carriers
- Pentacyclic Triterpenes
- Triterpenes
- gamma-Cyclodextrins
- gamma-cyclodextrin
- Betulinic Acid
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Topics |
- Animals
- Antineoplastic Agents
(administration & dosage, therapeutic use)
- Cell Cycle
(drug effects)
- Cell Line, Tumor
- Cell Proliferation
(drug effects)
- Drug Carriers
(chemistry)
- Female
- Melanoma
(drug therapy, pathology)
- Mice
- Mice, Inbred C57BL
- Pentacyclic Triterpenes
- Solubility
- Triterpenes
(administration & dosage, therapeutic use)
- X-Ray Diffraction
- gamma-Cyclodextrins
(chemistry)
- Betulinic Acid
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