Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content

Pharm Res. 2016 Dec;33(12):3031-3043. doi: 10.1007/s11095-016-2025-y. Epub 2016 Sep 6.

Abstract

Purpose: Aim was to formulate oil-in-water (O/W) microemulsion with a high volume ratio of complex natural oil, i.e. copaiba oil and low surfactant content. The strategy of formulation was based on (i) the selection of surfactants based on predictive calculations of chemical compatibility between their hydrophobic moiety and oil components and (ii) matching the HLB of the surfactants with the required HLB of the oil.

Method: Solubility parameters of the hydrophobic moiety of the surfactants and of the main components found in the oil were calculated and compared. In turn, required HLB of oils were calculated. Selection of surfactants was achieved matching their solubility parameters with those of oil components. Blends of surfactants were prepared with HLB matching the required HLB of the oils. Oil:water mixtures (15:85 and 25:75) were the titrated with surfactant blends until a microemulsion was formed.

Results: Two surfactant blends were identified from the predictive calculation approach. Microemulsions containing up to 19.6% and 13.7% of selected surfactant blends were obtained.

Conclusion: O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.

Keywords: HLB; copaiba oil; microemulsion; oil-in-water; solubility parameters.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical
  • Computer Simulation
  • Drug Carriers
  • Emulsions
  • Fabaceae / chemistry
  • Gas Chromatography-Mass Spectrometry
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Models, Chemical
  • Particle Size
  • Plant Oils / chemistry*
  • Solubility
  • Surface-Active Agents / chemistry*
  • Water / chemistry

Substances

  • Drug Carriers
  • Emulsions
  • Plant Oils
  • Surface-Active Agents
  • Water