Author/Authors :
Zadeh Mehrizi, Tahereh Department of Clinical Research - Pasteur Institute of Iran - Tehran, Iran , Mosaffa, Nariman Department of Medical Immunology - School of Medicine - Shahid Beheshti University of Medical Sciences - Tehran, Iran , Khamesipour, Ali Tehran University of Medical Sciences - Tehran, Iran , Haji Molla Hoseini, Mostafa Department of Medical Immunology - School of Medicine - Shahid Beheshti University of Medical Sciences - Tehran, Iran , Ebrahimi Shahmabadi, Hasan Department of Microbiology - Faculty of Medicine - Rafsanjan University of Medical Sciences - Rafsanjan, Iran , Shafiee Ardestani, Mehdi Department of Radiopharmacy - Faculty of Pharmacy - Tehran University of Medical Sciences - Tehran, Iran , Ramezani, Amitis Department of Clinical Research - Pasteur Institute of Iran - Tehran, Iran
Abstract :
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.
Keywords :
Anionic Linear Globular , Dendrimer (ALGD) , Antileishmanial , Betulinic acid , L. major , Solubility
