title: Influence of β-cyclodextrin on the Properties of Norfloxacin Form A.
abstract: Cyclodextrins are able to form host-guest complexes with hydrophobic molecules to result in the formation of inclusion complexes. The complex formation between norfloxacin form A and β-cyclodextrin was studied by exploring its structure affinity relationship in an aqueous solution and in the solid state. Kneading, freeze-drying, and physical mixture methods were employed to prepare solid complexes of norfloxacin and β-cyclodextrin. The solubility of norfloxacin significantly increased upon complexation with β-cyclodextrin as demonstrated by a solubility isotherm of the AL type along with the results of an intrinsic dissolution study. The complexes were also characterized in the solid stated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier-transform infrared (FT-IR) spectroscopy, X-ray diffractometry, scanning electron microscopy (SEM), and solid-state nuclear magnetic resonance (ssNMR) spectrometry. The thermal analysis showed that the thermal stability of the drug is enhanced in the presence of β-cyclodextrin. Finally, the microbiological studies showed that the complexes have better potency when compared with pure drug.
authors.affiliation: Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, Rodovia Araraquara-Jaú, km 1, CEP: 14801-902, Araraquara, São Paulo, Brazil, lczenith@gmail.com.
authors.forename: Lucas
authors.initials: L
authors.lastname: Chierentin
authors.forename: Claudia
authors.initials: C
authors.lastname: Garnero
authors.forename: Ana Karina
authors.initials: AK
authors.lastname: Chattah
authors.forename: Poonam
authors.initials: P
authors.lastname: Delvadia
authors.forename: Thomas
authors.initials: T
authors.lastname: Karnes
authors.forename: Marcela Raquel
authors.initials: MR
authors.lastname: Longhi
authors.forename: Hérida Regina Nunes
authors.initials: HR
authors.lastname: Salgado
mesh_terms: D002152:Calorimetry, Differential Scanning / Q000379:methods; D004339:Drug Compounding / Q000379:methods; D005612:Freeze Drying / Q000379:methods; D057927:Hydrophobic and Hydrophilic Interactions; D008855:Microscopy, Electron, Scanning / Q000379:methods; D009643:Norfloxacin / Q000737:chemistry*; D012995:Solubility; D012996:Solutions / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013678:Technology, Pharmaceutical / Q000379:methods; D014961:X-Ray Diffraction / Q000379:methods; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D012996:Solutions; D047392:beta-Cyclodextrins; C031215:betadex; D009643:Norfloxacin