Polyvinylpyrrolidone oral films of enrofloxacin: film characterization and drug release

Int J Pharm. 2014 Aug 25;471(1-2):146-52. doi: 10.1016/j.ijpharm.2014.05.033. Epub 2014 May 22.

Abstract

Enrofloxacin is a fluoroquinolone derivative used for treating urinary tract, respiratory and skin infections in animals. However, low solubility and low bioavailability prevented it from using on humans. Polyvinylpyrrolidone (PVP) is an inert, non toxic polymer with excellent hydrophilic properties, besides it can enhance bioavailability by forming drug polymer conjugates. With the aim of increasing solubility and bioavailability, enrofloxacin thin films were prepared using PVP as a polymer matrix. The obtained oral thin films exhibited excellent uniformity and mechanical properties. Swelling properties of the oral thin films revealed that the water uptake was enhanced by 21%. The surface pH has been found to be 6.8±0.1 indicating that these films will not cause any irritation to oral mucosa. FTIR data of the oral thin films indicated physical interaction between drug and polymer. SEM analysis revealed uniform distribution of drug in polymer matrix. In vitro drug release profiles showed enhanced release profiles (which are also pH dependant) for thin films compared to pure drug. Antibacterial activity was found to be dose dependent and maximum susceptibility was found on Klebsiella pneumonia making this preparation more suitable for respiratory infections.

Keywords: Antibacterial activity; Controlled drug release; Enrofloxacin; Oral films; Solubility.

MeSH terms

  • Administration, Oral
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Calorimetry, Differential Scanning
  • Dose-Response Relationship, Drug
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Enrofloxacin
  • Fluoroquinolones / administration & dosage*
  • Fluoroquinolones / chemistry
  • Fluoroquinolones / pharmacology
  • Gram-Negative Bacteria / drug effects
  • Gram-Negative Bacteria / growth & development
  • Gram-Positive Bacteria / drug effects
  • Gram-Positive Bacteria / growth & development
  • Microscopy, Electron, Scanning
  • Povidone / chemistry*
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Surface Properties

Substances

  • Anti-Bacterial Agents
  • Drug Carriers
  • Fluoroquinolones
  • Enrofloxacin
  • Povidone