Binary and Ternary Complexes of Arteether β-CD - Characterization, Molecular Modeling and in Vivo Studies英文文献资料.docVIP

Pharmacology Pharmacy, 2011, 2, 212-225 doi:10.4236/pp.2011.23030 Published Online July 2011 (/journal/pp) Binary and Ternary Complexes of Arteether β-CD—Characterization, Molecular Modeling and in Vivo Studies Renu Chadha , Sushma Gupta , Natasha Pathak , Geeta Shukla , Dharamvir Singh Jain , 1* 1 1 2 3 4 4 Raghuvir R. S. Pissurlenkar , Evans C. Coutinho 1 University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India; 2 Department of Microbiology, Panjab Uni- Department of Pharmaceutical Chem- versity, Chandigarh, India; Department of Chemistry, Panjab University, Chandigarh, India; 3 4 istry, Bombay College of Pharmacy, Mumbai, India. Email: renukchadha@ Received April 10 , 2010; revised May 30 , 2011; accepted June 22 , 2010. th th nd ABSTRACT The purpose of the present work is to improve the antimalarial activity of arteether through enhancing its solubility subsequently bioavailability by incorporating the drug into the cyclodextrins cavity. The effect of hydrophilic polyvinyl propylene (PVP) polymer on the complexation and solubilizing efficiencies of cyclodextrins (CDs) is also elucidated. Inclusion of arteether molecule in solid state was evidenced by Differential scanning calorimeter (DSC), Powder X-ray diffractometery (PXRD), and in solution state by NMR and solution calorimetry. A 1:1 stoichiometry was proposed by the phase solubility studies both in presence and absence of PVP. The most plausibe mode of inclusion of arteether into the CD cavity is revealed by molecular modeling studies utalizing Fast Rigid Exhaustive Docking acronym. Solut