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 (R) 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 (R) 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-IAldeloaded enteric MP will be useful to investigate novel postbiotic-based treatments in different therapeutic areas. (c) 2018 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.