title: Characterization and evaluation of synthetic riluzole with β-cyclodextrin and 2,6-di-O-methyl-β-cyclodextrin inclusion complexes.
abstract: β-Cyclodextrin (β-CD) and 2,6-di-O-methyl-β-cyclodextrin (DM-β-CD) inclusion complexes with riluzole (RLZ) were prepared to improve water solubility and broaden potential pharmaceutical applications. CDs/RLZ inclusion complexes were confirmed via phase solubility studies, FT-IR spectroscopy, PXRD, DSC, (1)H NMR, and SEM. Phase solubility studies indicated that β-CD and DM-β-CD can form 1:1 inclusion complexes with RLZ, and the stability constants were 663.17 and 1609.07M(-1), respectively. Water solubility and dissolution rate of RLZ were significantly improved in complex forms, implying that the inclusion complexes may develop pharmaceutical applications. Preliminary in vitro cytotoxicity assay also showed that RLZ hepatotoxicity was not increased in the inclusion complexes.
authors.affiliation: College of Chemical Engineering, Sichuan University, No. 24 South Section 1, Yihuan Road, Chengdu 610065, PR China.
authors.forename: Lili
authors.initials: L
authors.lastname: Wang
authors.affiliation: College of Chemical Engineering, Sichuan University, No. 24 South Section 1, Yihuan Road, Chengdu 610065, PR China.
authors.forename: Shanshan
authors.initials: S
authors.lastname: Li
authors.affiliation: College of Chemical Engineering, Sichuan University, No. 24 South Section 1, Yihuan Road, Chengdu 610065, PR China.
authors.forename: Peixiao
authors.initials: P
authors.lastname: Tang
authors.affiliation: College of Chemical Engineering, Sichuan University, No. 24 South Section 1, Yihuan Road, Chengdu 610065, PR China.
authors.forename: Jin
authors.initials: J
authors.lastname: Yan
authors.affiliation: College of Chemical Engineering, Sichuan University, No. 24 South Section 1, Yihuan Road, Chengdu 610065, PR China.
authors.forename: Kailin
authors.initials: K
authors.lastname: Xu
authors.affiliation: College of Chemical Engineering, Sichuan University, No. 24 South Section 1, Yihuan Road, Chengdu 610065, PR China. Electronic address: lihuilab@sina.com.
authors.forename: Hui
authors.initials: H
authors.lastname: Li
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D011208:Powders; D066244:Proton Magnetic Resonance Spectroscopy; D019782:Riluzole / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013816:Thermodynamics; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D011208:Powders; D047392:beta-Cyclodextrins; C038119:heptakis(2,6-O-dimethyl)beta-cyclodextrin; D019782:Riluzole; C031215:betadex
keywords: 2 ;6-Di-O-methyl-β-cyclodextrin; 2,6-Di-O-methyl-β-cyclodextrin (PubChem CID: 10171019); Dimethyl sulfoxide (PubChem CID: 679); Ethanol (PubChem CID: 702); Hepatotoxicity; Inclusion complex; Methanol (PubChem CID: 887); Riluzole; Riluzole (PubChem CID: 5070); Solubilization; β-Cyclodextrin; β-Cyclodextrin (PubChem CID: 444041)