Metronidazole and Pentoxifylline films for the local treatment of chronic periodontal pockets: preparation, in vitro evaluation and clinical assessment

Expert Opin Drug Deliv. 2014 Jun;11(6):855-65. doi: 10.1517/17425247.2014.897325. Epub 2014 Mar 18.

Abstract

Objective: Periodontitis is one of the most important chronic inflammatory dental diseases arising from the destructive actions caused by a variety of pathogenic organisms presented in the oral cavity. The aim of this study is the preparation and in vitro evaluation of films for the local treatment of periodontal pockets.

Methods: The prepared films contained either metronidazole (Mtr), for its antimicrobial effect in periodontal diseases, using a mixture of polymers namely hydroxypropyl methyl cellulose, Carbopol 934 or locally applied Pentoxifylline (PTX), for its anti-inflammatory activity, using chitosan. All films were prepared using solvent casting technique and were evaluated for their physical characteristics, drug content uniformity, surface pH, swelling behavior, mechanical properties and in vitro release. Further characterization was done on the selected formulations using differential scanning calorimetry and scanning electron microscopy for surface structure. Clinical evaluation tests were also performed.

Result: Appropriate physical characteristics and mechanical properties for most formulations and their suitability for periodontal application were observed. In vitro drug release from most films showed a burst release rate for both Mtr and PTX during the first 2 h after which the release rate was markedly decreased. Clinical trials on patients revealed the advantageous use of Mtr and PTX as an adjunct treatment with traditionally used dental techniques.

Conclusion: The effectiveness of the co-therapy of either drug could add benefit in the eradication of chronic periodontal hazards.

Keywords: chitosan; clinical assessment; hydroxypropyl methyl cellulose; in vitro release; local drug delivery; metronidazole; pentoxifylline; solvent casting technique.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylates / chemistry
  • Adult
  • Anti-Infective Agents / administration & dosage*
  • Anti-Infective Agents / chemistry
  • Calorimetry, Differential Scanning
  • Chitosan / chemistry
  • Delayed-Action Preparations
  • Drug Delivery Systems*
  • Female
  • Humans
  • Hydrogen-Ion Concentration
  • Hypromellose Derivatives
  • Male
  • Methylcellulose / analogs & derivatives
  • Methylcellulose / chemistry
  • Metronidazole / administration & dosage*
  • Metronidazole / chemistry
  • Microscopy, Electron, Scanning
  • Middle Aged
  • Pentoxifylline / administration & dosage*
  • Pentoxifylline / chemistry
  • Periodontal Pocket / drug therapy*
  • Periodontal Pocket / metabolism
  • Platelet Aggregation Inhibitors / administration & dosage*
  • Platelet Aggregation Inhibitors / chemistry

Substances

  • Acrylates
  • Anti-Infective Agents
  • Delayed-Action Preparations
  • Platelet Aggregation Inhibitors
  • Metronidazole
  • Hypromellose Derivatives
  • Methylcellulose
  • Chitosan
  • carbopol 934P
  • Pentoxifylline