Effect of ethylcellulose and propylene glycol on the controlled-release performance of glyceryl monooleate-mertronidazole periodontal gel

Pharm Dev Technol. 2015 Mar;20(2):159-68. doi: 10.3109/10837450.2013.852573. Epub 2013 Nov 21.

Abstract

Controlled-release metronidazole, mucoadhesive gel proposed as a drug-delivery system for periodontal application was developed and characterized. The system was based on a mixture of glycerylmonooleate (GMO) and ethylcellulose (EC). The mechanism of release depends: firstly, on the ability of GMO to form a viscous liquid crystalline mesophases and secondly on the solubilized EC to form a hydrophobic network when the mixture comes into contact with water resulting in sustaining the release of the drug. Ethylcellulose dissolved in GMO had a profound influence on the rate of drug release, reduced the initial drug release and prolonged the sustained release of metronidazole. Propylene glycol (PG) was added to increase the solubility of the drug and water was added with PG to control the viscosity. A controlled release formulation containing w/w, 20% metronidazole, 10% PG, 5% water and 65% GMO that contains 7% EC was found to be mucoadhesive, easily injectable at room temperature, and to follow Fickian diffusion release mechanism. When the drug loading was increased the drug release was accelerated, and the mechanism followed anomalous controlled-release mechanism. Stability studies indicated that the formulation should be stored at 4 °C in a dark place.

Keywords: Liquid crystals; metronidazole gel; mucoadhesive; periodontal; pharmaceutical gel.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adhesiveness
  • Animals
  • Anti-Infective Agents / administration & dosage
  • Anti-Infective Agents / chemistry*
  • Cellulose / analogs & derivatives*
  • Cellulose / chemistry
  • Chickens
  • Delayed-Action Preparations
  • Drug Delivery Systems
  • Drug Liberation
  • Drug Stability
  • Drug Storage
  • Excipients / chemistry*
  • Gels
  • Glycerides / chemistry*
  • Humans
  • Metronidazole / administration & dosage
  • Metronidazole / chemistry*
  • Mucous Membrane / drug effects
  • Particle Size
  • Periodontal Diseases / drug therapy
  • Phase Transition
  • Propylene Glycol / chemistry*
  • Rheology
  • Solubility

Substances

  • Anti-Infective Agents
  • Delayed-Action Preparations
  • Excipients
  • Gels
  • Glycerides
  • Metronidazole
  • Propylene Glycol
  • ethyl cellulose
  • Cellulose
  • monoolein