Development of Novel Indole-3-Aldehyde-Loaded Gastro-Resistant Spray-Dried Microparticles for Postbiotic Small Intestine Local Delivery

Considering the recent evidence on the therapeutic potential of postbiotics, this study focused on 2 main goals: (1) to develop an enteric microparticle (MP) formulation for intestinal localized delivery of indole-3-aldehyde (3-IAld) (a microbial-derived metabolite produced by the host's lactobacilli during the catabolic pathway of tryptophan) and (2) to provide support in the employment of spray-drying as innovative one-step manufacturing technique for enteric products. For this purpose, special attention was taken in the knowledge of the influence of equipment setup and feedstock properties on MP enteric behavior. Eudragit^® S100 and L100 and ethyl cellulose were used as wall materials and NaOH and ethanol solutions as solvent systems. 3-IAld loading was maintained at 10% w/w. As postulated, feedstock properties influenced spray-drying regime. In addition, they prevailed over other spray-drying process factors in determining MP enteric behavior. Albeit the high buckling regime that produced crumped particles, gastro resistance was obtained by spray-drying 2:1 Eudragit^® S100:L100 with 30% w/w ethyl cellulose in ethanol solution. These results support the use of spray-drying as a method for manufacturing gastro-resistant MP. The obtained 3-IAld-loaded enteric MP will be useful to investigate novel postbiotic-based treatments in different therapeutic areas.