Clove oil based co-surfactant free microemulsion of flurbiprofen: Improved solubility with ameliorated drug-induced gastritis

Pak J Pharm Sci. 2019 Nov;32(6(Supplementary)):2787-2793.

Abstract

Flurbiprofen, an NSAID, is a water insoluble drug that is also notorious for gastric irritation and inflammation. This study was aimed at using a natural gastrprotective oil as the internal phase to develop flurbiprofen micro emulsion (ME) to improve it solubility and ameliorate its gastric side effects. Upon screening of ME components for drug solubility, clove oil, tween 80 and transcutol were identified as the oil, surfactant and co surfactant, respectively, with higher flurbiprofen solubility. Pseudo-ternary phase diagrams revealed that the ME made with surfactant only and without co-surfactant displayed the similar ME region as made with the mixture of surfactant and co-surfactant. Furthermore, drug loaded oil was also used to draw pseudo-ternary phase diagram and a very little decrease in the ME region was observed. Therefore, co-surfactant free flurbiprofen loaded ME was developed to avoid side effects associated with the use of excessive surfactant quantities. ME were found to possess size in the range of 11-41 nm with PDI <0.5 and a slightly negative charge. Conductivity, pH and refractive indices of the selected MEs were well in the range. Drug release studies indicated maximum drug release from MEs within 5 min. Analysis of the gastric mucosa of rats after oral administration of drug solution and drug loaded ME confirmed that clove oil based ME provided significant protection against the NSAIDs induced gastric damage.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / adverse effects
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Chemistry, Pharmaceutical / methods
  • Clove Oil / chemistry*
  • Drug Liberation / drug effects
  • Emulsions / chemistry*
  • Flurbiprofen / chemistry*
  • Gastritis / chemically induced
  • Gastritis / prevention & control*
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Polysorbates / chemistry
  • Rats
  • Surface-Active Agents / chemistry*
  • Water / chemistry

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Clove Oil
  • Emulsions
  • Polysorbates
  • Surface-Active Agents
  • Water
  • Polyethylene Glycols
  • Flurbiprofen