Genistein encapsulated inulin-stearic acid bioconjugate nanoparticles: Formulation development, characterization and anticancer activity.

Abstract

Achieving controlled and site-specific delivery of hydrophobic drugs in the colon environment is a major challenge. The primary goal of this research was to synthesize inulin-stearic acid (INU-SA) conjugate and to evaluate its potential in the site-specific delivery of genistein (GEN) for the treatment of colon cancer. INU is a hydrophilic polysaccharide biological macromolecule was modified with hydrophobic SA to form amphiphilic conjugate (INU-SA) which can self-assemble into spherical nanoparticles with interesting drug release properties. The hydrophobic GEN was encapsulated into the INU-SA conjugate to prepare GEN loaded nanoparticles (GNP). The prepared GNP possessed nano size (115 nm), good colloidal dispersibility (0.066 PDI), and high drug encapsulation efficiency (92.2%). The release behaviour of GNP indicated the site-specific release of GEN, only 3.4% at gastric pH while 94% at intestinal pH. The prepared GNP showed potential cytotoxicity against HCT 116 human colorectal cancer cells, as demonstrated by antiproliferation and apoptosis assays. The observed half maximum inhibitory concentration (IC50) value of GNP (5.5 μg/mL) was significantly lower than pure GEN (28.2 μg/mL) due to higher cellular internalization of GNP than free GEN. Therefore, this research suggests a way to improve the therapeutic effectiveness of natural biomolecules using modified and biocompatible polysaccharide INU.

• Authors: Ashok Kumar Jangid, Raghu Solanki, Sunita Patel, Deep Pooja, Hitesh Kulhari
• Journal: International journal of biological macromolecules (Int J Biol Macromol) Vol. 206 Pg. 213-221 (May 01 2022) ISSN: 1879-0003 [Electronic] Netherlands
• PMID: 35181329 (Publication Type: Journal Article)
• Copyright: Copyright © 2022. Published by Elsevier B.V.

Chemical References

• Drug Carriers
• Polysaccharides
• Stearic Acids
• stearic acid
• Inulin
• Genistein

Topics

• Drug Carriers (chemistry)
• Genistein (pharmacology)
• Humans
• Inulin (chemistry)
• Nanoparticles (chemistry)
• Polysaccharides
• Stearic Acids