PHYSICO-CHEMICAL AND TOXICOLOGICAL
EVALUATIONS OF BETULIN AND BETULINIC
ACID INTERACTIONS WITH HYDROPHILIC
CYCLODEXTRINS.
CODRUŢA M. ŞOICA1*, CAMELIA I. PEEV1, SORINA CIURLEA1,
RITA AMBRUS2, CRISTINA DEHELEAN1
1University of Medicine and Pharmacy Victor Babeş Timişoara, Faculty
of Pharmacy, Eftimie Murgu Square no.2, 300041, Timişoara, România
2University of Szeged, Faculty of Pharmacy, Hungary
*corresponding author: codrutasoica@yahoo.com
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Abstract:
Betulin and betulinic acid are pentacyclic triterpens with antitumor activity, especially on melanoma and skin cancer. Considering their low water solubility, studies have been conducted in order to improve this aspect. One possible solution is the preparation of inclusion complexes with semisynthetic cyclodextrins using different methods.
The purpose of this study was the evaluation of the stability constants of betulin and betulinic acid complexes with two cyclodextrins: hydroxypropyl-beta-cyclodextrin and randomly methylated-beta-cyclodextrin, using the Higuchi and Connors phase solubility method. Products have been analyzed by scanning electron microscopy and in vitro tests. The presence of cyclodextrins increases water solubility and biological activity without toxic
activity.
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