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Biodegradable, bile salt microparticles for localized fat dissolution.

Hanieh SafariNicholas KaczorowskiMichael L FelderEmma R BrannonMita VargheseKanakadurga SingerOmolola Eniola-Adefeso
Published in: Science advances (2020)
Bile acids are proposed as therapeutic agents for various diseases, including liver diseases and obesity. However, oral or subcutaneous administration of a solubilized version of these drugs has limited efficacy and imposes unwanted side effects. Here, we describe a gold-templating method for fabricating stable, bile salt-cholate or deoxycholate-microparticles. The gold ions' reduction at the oil-water interface in a double emulsion solvent evaporation process enables a gold-bile salt interaction and the formation of bile salt particles. We demonstrate that composite microparticles release cholate/deoxycholate into solution via a surface erosion process. We illustrate these particles' capability to lyse adipocytes, both in vitro and in vivo, with minimal side effects, contrary to the Food and Drug Administration-approved salt solution that leads to severe inflammation and ulceration. Overall, particle-based cholate/deoxycholate opens opportunities for localized delivery of these salts, improving efficacy while minimizing side effects associated with oral and subcutaneous use.
Keyphrases
  • drug administration
  • adipose tissue
  • type diabetes
  • oxidative stress
  • drug delivery
  • ionic liquid
  • insulin resistance
  • fatty acid
  • quantum dots
  • physical activity
  • skeletal muscle
  • human health