A Novel Nanoformulation for Reducing the Toxicity and Increasing the Efficacy of Betulinic Acid Using Anionic Linear Globular Dendrimer
نویسندگان
1 Department of Medical Immunology, School of Medicine, Shahid Beheshti University of Medical Sciences, Tehran, Iran
2 Department of Microbiology, Faculty of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan, Iran
3 Department of Radiopharmacy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
4 Department of Clinical Research, Pasteur Institute of Iran, Tehran, Iran
5 Department of Clinical Research, Pasteur Institute of Iran, Tehran, Iran
6 Center for Research and Training in Skin Diseases and Leprosy, Tehran University of Medical Sciences, Tehran, Iran
7 Department of Medical Immunology, School of Medicine, Shahid Beheshti University of Medical Sciences, Tehran, Iran
doi
10.22052/JNS.2021.01.016چکیده
Betulinic acid (BA) is an antileishmanial herbal drug with low solubility and high toxicity. To our knowledge, this is the first study in which betulinic acid is loaded into Anionic Linear Globular Dendrimer (ALGD) in order to resolve the toxicity and insolubility problem. In order to solve mentioned problems, BA was loaded into ALGD nanocarrier. The formulation was characterized in terms of chemical bonds and morphology using Fourier Transform Infrared (FTIR) Spectroscopy, Atomic Force Microscopy (AFM) and Proton Nuclear Magnetic Resonance (1HNMR) methods. According to our study insoluble BA could loaded well into ALGD. This loading caused an increase in the solubility rate of BA by more than 700-fold and a decrease in the toxicity effects to zero in vivo environment. Overall, BD at a dose of 40 mg/kg caused a significant decreased in the number of parasite (leishmania major (L. major)) in vitro and in vivo without inducing any toxic effect.
