Pickering nano-emulsion as a nanocarrier for pH-triggered drug release

Int J Pharm. 2018 Oct 5;549(1-2):299-305. doi: 10.1016/j.ijpharm.2018.07.066. Epub 2018 Jul 31.

Abstract

This study investigates the formulation of surfactant-free Pickering nano-emulsions able to release a drug at specific pH, in order to enhance its oral bioavailability. The stabilizing nanoparticles composed of magnesium hydroxide, were obtained by nano-precipitation method. The oil-in-water Pickering nano-emulsions stabilized with Mg(OH)2 nanoparticles, and encapsulating a model of hydrophobic drug (ibuprofen) were formulated following a high-energy process, using a sonication probe. The experimental approach explored the impact of all formulation parameters, composition and size of Mg(OH)2 nanoparticles, on the physico-chemical properties of the Pickering nano-emulsions. The system was characterized by DLS and transmission electron microscopy. In addition, Mg(OH)2 has the advantage of being solubilized in an acid medium leading to the destabilization of the nano-emulsion and the release of the active ingredient orally. The acid release study (pH = 1.2) showed cumulative release as a function of initial nanodroplet loading and saturation concentration. In basic media (pH = 6.8), we found a significant release of ibuprofen from the nano-emulsions that already had saturation in an acid medium. These nano-emulsions can not only protect patients from the side effects of acid medicines through the basic properties of hydroxides but also can contribute to the increase of the bioavailability of these drugs. In addition, once in the stomach pH is increased by hydroxides and promotes the release of active ingredients such as ibuprofen whose solubility is strongly influenced by pH.

MeSH terms

  • Administration, Oral
  • Cyclooxygenase Inhibitors / administration & dosage
  • Cyclooxygenase Inhibitors / chemistry*
  • Delayed-Action Preparations
  • Drug Carriers*
  • Drug Compounding
  • Drug Liberation
  • Drug Stability
  • Emulsions
  • Hydrogen-Ion Concentration
  • Hydrophobic and Hydrophilic Interactions
  • Ibuprofen / administration & dosage
  • Ibuprofen / chemistry*
  • Kinetics
  • Magnesium Oxide / chemistry*
  • Nanoparticles*
  • Nanotechnology*
  • Solubility
  • Technology, Pharmaceutical / methods*

Substances

  • Cyclooxygenase Inhibitors
  • Delayed-Action Preparations
  • Drug Carriers
  • Emulsions
  • Magnesium Oxide
  • Ibuprofen