Colonic delivery of pelargonidin-3-O-glucoside using pectin-chitosan-nanoliposome: Transport mechanism and bioactivity retention

Int J Biol Macromol. 2020 Sep 15:159:341-355. doi: 10.1016/j.ijbiomac.2020.05.076. Epub 2020 May 15.

Abstract

Colon-targeted delivery is an active area of research as it can improve drug stability, bioactivity, and lessen the systematic toxicity. In this study, the colon-specific delivery of pelargonidin-3-O-glucoside (P3G) was investigated using pectin (P)/chitosan (CH)-functionalized nanoliposome (NL). The food simulant stability, transport mechanism, and bioactivity retention potential of carrier systems were studied. Results showed that polymer-coated nanoliposomes (P-CH-NL and CH-NL) improved the thermal and food simulant stability as well as enhanced the P3G retention during the in vitro digestion. The maximum P3G retention after enzymatic and non-enzymatic digestion was observed by P-CH-NL and the values were 47.5% and 57.5%, respectively. However, all nanoliposomal carriers followed Fickian diffusion mechanism both in in vitro food simulants and in vitro digestion models. Digested functionalized nanoliposomes revealed higher antioxidant properties after gastric digestion. Following by simulated intestinal fluid digestion, ABTS antioxidant activity of P-CH-P3G-NL was 12.52% and 6.31% higher than that of P3G-NL and CH-P3G-NL, respectively, while DPPH scavenging capacity of P-CH-P3G-NL was 5.57% and 1.86% greater than that of P3G-NL and CH-P3G-NL, respectively. Therefore, the developed functionalized nanoliposome can be useful for colon-targeted delivery and applicable in functional foods and/or beverages.

Keywords: Bioactivity retention; Chitosan; Nanoliposome; Pectin; Pelargonidin-3-O-glucoside; Transport mechanism.

MeSH terms

  • Algorithms
  • Anthocyanins / administration & dosage*
  • Anthocyanins / pharmacokinetics
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Chitosan / chemistry*
  • Colon / drug effects*
  • Colon / metabolism
  • Drug Carriers / chemistry*
  • Drug Delivery Systems
  • Drug Liberation
  • Drug Stability
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology
  • Intestinal Absorption
  • Kinetics
  • Liposomes / chemistry*
  • Models, Theoretical
  • Nanocomposites / chemistry*
  • Particle Size
  • Pectins / chemistry*
  • Temperature

Substances

  • Anthocyanins
  • Antioxidants
  • Drug Carriers
  • Hypoglycemic Agents
  • Liposomes
  • Pectins
  • pelargonidin-3-glucoside
  • Chitosan