Arabinoxylans-Based Oral Insulin Delivery System Targeting the Colon: Simulation in a Human Intestinal Microbial Ecosystem and Evaluation in Diabetic Rats

Ana L. Martínez-López*, Elizabeth Carvajal-Millan, Rafael Canett-Romero, Satya Prakash, Agustín Rascón-Chu, Yolanda L. López-Franco, Jaime Lizardi-Mendoza, Valerie Micard

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Arabinoxylans (AX) microcapsules loaded with insulin were prepared by enzymatic gelation of AX, using a triaxial electrospray method. The microcapsules presented a spherical shape, with an average size of 250 µm. The behavior of AX microcapsules was evaluated using a simulator of the human intestinal microbial ecosystem. AX microcapsules were mainly (70%) degraded in the ascending colon. The fermentation was completed in the descending colon, increasing the production of acetic, propionic, and butyric acids. In the three regions of the colon, the fermentation of AX microcapsules significantly increased populations of Bifidobacterium and Lactobacillus and decreased the population of Enterobacteriaceae. In addition, the results found in this in vitro model showed that the AX microcapsules could resist the simulated conditions of the upper gastrointestinal system and be a carrier for insulin delivery to the colon. The pharmacological activity of insulin-loaded AX microcapsules was evaluated after oral delivery in diabetic rats. AX microcapsules lowered the serum glucose levels in diabetic rats by 75%, with insulin doses of 25 and 50 IU/kg. The hypoglycemic effect and the insulin levels remained for more than 48 h. Oral relative bioavailability was 13 and 8.7% for the 25 and 50 IU/kg doses, respectively. These results indicate that AX microcapsules are a promising microbiota-activated system for oral insulin delivery in the colon.

Original languageEnglish
Article number1062
JournalPharmaceuticals
Volume15
Issue number9
DOIs
StatePublished - Sep 2022

Bibliographical note

Funding Information:
This research was supported by Fondo Sectorial de Investigación en Salud y Seguridad Social SSA/IMSS/ISSSTE-CONACYT, México (grant 179746 to E. Carvajal-Millan).

Publisher Copyright:
© 2022 by the authors.

Keywords

  • SHIME
  • bioavailability
  • colon
  • electrospray
  • insulin
  • oral drug delivery

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