Highly cross-linked arabinoxylans microspheres as a microbiota-activated carrier for colon-specific insulin delivery

Eur J Pharm Biopharm. 2021 Jun:163:16-22. doi: 10.1016/j.ejpb.2021.02.014. Epub 2021 Mar 24.

Abstract

In vivo evaluation of arabinoxylans (AX) microspheres showed to protect insulin from degradation in the upper gastrointestinal tract and carrier insulin to colon. Insulin-loaded AX microspheres (50 UI/kg) decreased blood glucose level by 39% in diabetic rats with a maximum effect at 18 h post-administration, indicating that insulin remains bioactive. The continuous administration (4 days) of insulin-loaded AX microspheres improved the polyuria and increased the production of short-chain fatty acids, as well as Bifidobacterium and Bacteroides in diabetic rats compared to untreated diabetic rats. AX microspheres are a potential microbiota-activated carrier for colon-specific drug delivery and could be useful as a complementary treatment for diabetes.

Keywords: Arabinoxylans; Colon-targeted; Drug-delivery; Insulin carrier; Microspheres.

MeSH terms

  • Administration, Oral
  • Animals
  • Colon / metabolism
  • Colon / microbiology
  • Diabetes Mellitus, Experimental / chemically induced
  • Diabetes Mellitus, Experimental / drug therapy
  • Diabetes Mellitus, Experimental / microbiology
  • Diabetes Mellitus, Type 1 / chemically induced
  • Diabetes Mellitus, Type 1 / drug therapy*
  • Diabetes Mellitus, Type 1 / microbiology
  • Diabetes Mellitus, Type 2 / chemically induced
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / microbiology
  • Drug Carriers / metabolism*
  • Gastrointestinal Microbiome*
  • Humans
  • Insulin / administration & dosage*
  • Insulin / pharmacokinetics
  • Intestinal Mucosa / metabolism
  • Intestinal Mucosa / microbiology
  • Male
  • Microspheres
  • Rats
  • Streptozocin / administration & dosage
  • Streptozocin / toxicity
  • Xylans / metabolism*

Substances

  • Drug Carriers
  • Insulin
  • Xylans
  • Streptozocin
  • arabinoxylan