Novel microemulsion-based gels for topical delivery of indomethacin: Formulation, physicochemical properties and in vitro drug release studies

J Colloid Interface Sci. 2017 Dec 1:507:323-336. doi: 10.1016/j.jcis.2017.08.011. Epub 2017 Aug 4.

Abstract

Hypothesis: Microemulsion-based semisolid systems may be considered as an interesting alternative to the traditional dosage forms applied in topical drug delivery. Mechanical properties of topical products are important both in terms of application and dosage form effectiveness. In this study we designed and evaluated novel microemulsion-based gels with indomethacin and analyzed the factors affecting their mechanical characteristics and drug release.

Experiments: The impact of the microemulsion composition on the extent of isotropic region was investigated with the use of pseudoternary phase diagrams. Selected microemulsions were analyzed in terms of electrical conductivity and surface tension in order to determine the microemulsion type. Microemulsions were transformed into polymer-based gels and subjected to rheological and textural studies. Finally, the indomethacin release from the analyzed gels was studied and compared to commercially available product.

Findings: The extent of isotropic domain in pseudoternary phase diagrams seems to be dependent on the polarity of the oil phase. The surface tension and conductivity monitored as a function of water content in microemulsion systems revealed possible structural transformations from w/o through bicontinuous systems into o/w. The mechanical properties of semisolid microemulsion-based systems depended on the composition of surface active agents and the drug presence. The drug release profiles observed in the case of the investigated gels differed from those recorded for the commercially available product which was most probably caused by the different structure of both systems.

Keywords: Gel; In vitro drug release; Indomethacin; Microemulsion; Rheology; Texture profile analysis.

MeSH terms

  • Administration, Topical
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Drug Carriers / chemistry*
  • Drug Compounding
  • Drug Liberation
  • Emulsions / chemistry*
  • Gels / chemistry*
  • Hydrogen-Ion Concentration
  • Indomethacin / administration & dosage
  • Indomethacin / chemistry*
  • Particle Size
  • Polymers / chemistry
  • Solubility
  • Surface Properties
  • Surface-Active Agents / chemistry
  • Viscosity

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Emulsions
  • Gels
  • Polymers
  • Surface-Active Agents
  • Indomethacin