title: Investigation of β-cyclodextrin-norfloxacin inclusion complexes. Part 1. Preparation, physicochemical and microbiological characterization.
abstract: BACKGROUND
  Drugs classified as class IV by the Biopharmaceutical Classification System present significant problems in relation to effective oral administration. In the case of antibiotics, the subsequently high doses required can enhance the emergence of microorganism resistance and lead to a low rate of patient treatment adherence.
  
  
  OBJECTIVE
  In an attempt to improve physicochemical properties and microbiological activity of norfloxacin, the aim of this study was to investigate different methods (coevaporation, kneading followed by freeze-drying or spray-drying) to obtain complexes of norfloxacin and different cyclodextrins.
  
  
  METHODS
  Guest-host interactions were investigated through a complete physical-chemical characterization and the dissolution profile and microbiological activity were determined.
  
  
  RESULTS
  The formation of a complex of norfloxacin and β-cyclodextrin (1:1), obtained by kneading followed by freeze drying, led to increased drug solubility, which could maximize the oral drug absorption.
  
  
  CONCLUSIONS
  Moreover, the microbiological activity was enhanced by around 23.3%, demonstrating that the complex formed could represent an efficient drug delivery system.
authors.affiliation: Department of Pharmaceutical Sciences, Health Science Centre, Federal University of Santa Catarina, Quality Control Laboratory, J/K 207, 88040-900, Florianópolis-SC, Brazil.
authors.forename: Cassiana
authors.initials: C
authors.lastname: Mendes
authors.forename: Bárbara Paula
authors.initials: BP
authors.lastname: Wiemes
authors.forename: Aline
authors.initials: A
authors.lastname: Buttchevitz
authors.forename: Ana Paula
authors.initials: AP
authors.lastname: Christ
authors.forename: Karla Giacomelli
authors.initials: KG
authors.lastname: Ribas
authors.forename: Andréa Inês Horn
authors.initials: AI
authors.lastname: Adams
authors.forename: Marcos Antônio Segatto
authors.initials: MA
authors.lastname: Silva
authors.forename: Paulo Renato
authors.initials: PR
authors.lastname: Oliveira
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D004055:Differential Thermal Analysis / Q000379:methods; D004337:Drug Carriers; D004355:Drug Stability; D008855:Microscopy, Electron, Scanning / Q000379:methods; D009643:Norfloxacin / Q000737:chemistry* / Q000494:pharmacology; D004364:Pharmaceutical Preparations; D011199:Potentiometry / Q000379:methods; D033362:Powder Diffraction; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013212:Staphylococcus epidermidis / Q000187:drug effects; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D004364:Pharmaceutical Preparations; D047392:beta-Cyclodextrins; D009643:Norfloxacin
keywords: inclusion complex; microbiological activity; norfloxacin; solubility; β-cyclodextrin