Biodegradable, bile salt microparticles for localized fat dissolution

Abstract

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.

The Role of Fat Reducing Agents on Adipocyte Death and Adipose Tissue Inflammation

“…Recent studies have remained consistent with previous reports, showing that DCA induces inflammatory cell death and that DCA is non-selective for adipocytes. Specifically, vascular injury was noted at higher dose concentrations (2% and 4%) which is consistent with Schuller-Petrovic et al.’s findings above ( 37 , 38 ).…”

Supervised learning model predicts protein adsorption to carbon nanotubes

“…Engineered nanoparticles are poised to transform how we undertake biological sensing ( 1 , 2 ), imaging ( 3 , 4 ), and delivery ( 5 – 7 ): Nanoscale materials enable localization within otherwise inaccessible biological environments and exhibit highly tunable physicochemical properties to tailor function. Different nanoparticle platforms offer application-dependent advantages, such as near-infrared fluorescent nanoparticles for through-tissue imaging ( 8 , 9 ) or biodegradable nanoparticles for in vivo delivery ( 10 – 12 ). In particular, single-walled carbon nanotubes (SWCNTs) are well suited for biological sensing and imaging due to their tissue-transparent and photostable near-infrared fluorescence, in addition to their readily modifiable surface ( 13 – 15 ).…”

Biophysical and genetic cues regulating the structural remodeling of adipose tissue upon caloric excess

“…Bile acids (BAs) are natural detergents of the body known to emulsify fat and form micelles to promote solubilization and absorption 6 . Recently, BA-loaded microparticles were proposed as an alternative to invasive liposuction for the removal of undesired fat deposits 7 . Moreover, the role of BAs as signaling molecules that activate cell surface and nuclear receptors has been well established 8,9 .…”