title: Enhanced dissolution and stability of lansoprazole by cyclodextrin inclusion complexation: preparation, characterization, and molecular modeling.
abstract: In this study, lansoprazole (LSP)/cyclodextrin (CD) inclusion complexes were prepared using a fluid bed coating technique, with β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (HPCD) as the host molecules, respectively, to simultaneously improve the dissolution and stability of LSP. The dissolution rate and stability of LSP was dramatically enhanced by inclusion complexation regardless of CD type. LSP/HPCD inclusion complex was more stable under illumination than LSP/β-CD inclusion complex. Differential scanning calorimetry and powder X-ray diffractometry proved the absence of crystallinity in both LSP/CD inclusion complexes. Fourier transform infrared spectroscopy together with molecular modeling indicated that the benzimidazole of LSP was included in the cavity of both CDs, while LSP was more deeply included in HPCD than β-CD. The enhanced photostability was due to the inclusion of the sulfinyl moiety into the HPCD cavity. CD inclusion complexation could improve the dissolution and stability of LSP.
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of Ministry of Education and PLA, Fudan University, Shanghai, 201203, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Lu
authors.forename: Tao
authors.initials: T
authors.lastname: Guo
authors.forename: Jianping
authors.initials: J
authors.lastname: Qi
authors.forename: Jiwen
authors.initials: J
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000737:chemistry*; D001562:Benzimidazoles / Q000737:chemistry; D002152:Calorimetry, Differential Scanning / Q000379:methods; D004355:Drug Stability; D064747:Lansoprazole; D008958:Models, Molecular; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D001562:Benzimidazoles; D047392:beta-Cyclodextrins; D064747:Lansoprazole; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C031000:benzimidazole