(240g) A Gold-Templating Method for Fabrication of Bile Salt-Based Composite Microparticles with Controlled Geometry for Localized Fat Dissolution (INVITED SPEAKER)

Bile acids and their salts are proposed as therapeutic agents for various diseases, including bile synthesis disorders, liver diseases, and obesity. However, oral or subcutaneous administration of a solubilized version of these drugs can limit their efficacy and impose unwanted side effects. Here, we describe a gold-templating method for fabricating stable, bile salts – cholate or deoxycholate – microparticles. The reduction of gold ions at the oil-water interface in a double emulsion solvent evaporation process enables a gold-bile salt interaction, leading to the formation of bile salt particles. We demonstrated that composite microparticles release cholate/deoxycholate via a surface erosion process, and the size of the particles was linked to the bile salt concentration in the water phase. Importantly, the bile salt particles lyse adipocytes, both in vitro and in vivo, with minimal side effects, contrary to the FDA approved salt solution that leads to severe inflammation and ulceration. Finally, we show that bile salt-based particles can be loaded with drugs, using rhodamine as a model, allowing for co-administration of the released bile salt with other therapeutic agents. Overall, particle-based cholate/deoxycholate can open opportunities for localized delivery of these salts, which can improve efficacy while minimizing side effects associated with oral and subcutaneous use.