Nanocapsules improve indole-3-carbinol photostability and prolong its antinociceptive action in acute pain animal models

Eur J Pharm Sci. 2018 Jan 1:111:133-141. doi: 10.1016/j.ejps.2017.09.050. Epub 2017 Sep 28.

Abstract

This study aimed the development of nanocapsules (NCs) for oral indole-3-carbinol (I3C) administration and evaluation of antinociceptive potential of this compound in its two forms, free and nanoencapsulated, using acute pain models. NCs showed adequate physicochemical characteristics and protected the I3C against UVC radiation exposure. It was observed no chemical bond between I3C and polymer by FTIR. Besides, X-ray and DSC analysis suggested that I3C was molecularly dispersed in NCs. The dialysis bag technique showed that almost 100% of the compound was released from NCs at 360min. Mathematical modeling demonstrated that this release occurred in two rates, with an initial burst effect followed by a slower release of I3C. Regarding the in vivo analysis, time-response curve showed that both forms of I3C caused an inhibition in inflammatory phase of nociception induced by formalin and increased the latency response in hot plate test. Interestingly, NCs were able to prolong the I3C effect in both tests. Furthermore, in dose-response curve, only I3C in its nanoencapsulated form presented effect on inflammatory phase of the formalin test. In conclusion, NCs to I3C incorporation presented adequate nanometric characteristics and prolonged its antinociceptive action in acute pain models tested.

Keywords: Cruciferous vegetable metabolites; Diindolylmethane; Formalin test; Nanoparticles; Pain; Vegetable oil.

MeSH terms

  • Analgesics / administration & dosage*
  • Analgesics / radiation effects
  • Analgesics / therapeutic use
  • Animals
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Carriers / chemistry*
  • Drug Stability
  • Indoles / administration & dosage*
  • Indoles / radiation effects
  • Indoles / therapeutic use
  • Inflammation
  • Male
  • Mice
  • Nanocapsules / chemistry*
  • Pain / drug therapy*
  • Pain / immunology
  • Particle Size
  • Surface Properties
  • Ultraviolet Rays*

Substances

  • Analgesics
  • Drug Carriers
  • Indoles
  • Nanocapsules
  • indole-3-carbinol