Visualisation of real-time oral biodistribution of fluorescent labeled self-microemulsifying drug delivery system of olmesartan medoxomil using optical imaging method

Drug Metab Pharmacokinet. 2021 Feb:36:100365. doi: 10.1016/j.dmpk.2020.10.004. Epub 2020 Oct 29.

Abstract

In the present study, the biodistribution of self-microemulsifying drug delivery system of hydrophobic olmesartan medoxomil (OM-SMEDDS) was determined by labeling with a fluorescent dye VivoTag®680 XL and Xenolight® DiR. Labeled OM-SMEDDS and control dye solution administered orally to mice; real-time dynamic biodistributions over 7 h were determined by 2D-fluorescent imaging to verify their anatomic location. Fluorescent Emissions by Vivotag 680® XL and Xenolight® DiR labeled OM-SMEDDS emitted 2 to 24 times stronger emission than control dye administered group. To further confirm the results, organs were removed and examined using the same technique at the end of 7 h. VivoTag®680XL and Xenolight® DiR emitted 4 and 1.7 times stronger emission respectively than control dye administered mice in ex-vivo organ imaging studies. This study showed that OM-SMEDDS can be succesfully labeled with fluorescent dye and tracked with optical imaging method for the visualisation of biodistribution of drugs and is also useful for enhanced bioavailability.

Keywords: Biodistribution; Near infrared (NIR); Olmesartan; Optical imaging; Pharmacokinetics; Real-time fluorescent imaging; SMEDDS; Vivotag; Xenolight.

MeSH terms

  • Administration, Oral
  • Animals
  • Drug Delivery Systems / methods*
  • Emulsifying Agents / administration & dosage
  • Emulsifying Agents / analysis
  • Emulsifying Agents / metabolism*
  • Fluorescent Dyes / administration & dosage
  • Fluorescent Dyes / analysis
  • Fluorescent Dyes / metabolism*
  • Male
  • Mice
  • Olmesartan Medoxomil / administration & dosage
  • Olmesartan Medoxomil / analysis
  • Olmesartan Medoxomil / metabolism*
  • Optical Imaging / methods*
  • Solubility / drug effects
  • Tissue Distribution / drug effects
  • Tissue Distribution / physiology

Substances

  • Emulsifying Agents
  • Fluorescent Dyes
  • Olmesartan Medoxomil