Scientists have created an entirely new drug delivery system for the anticancer tyrosine kinase inhibitor regorafenib (REG) using a biocompatible inulin platform that not only significantly improves the pharmacokinetics of the drug with or without food, but also modulates the gut microbiome to improve immune responses and reduce tumor burden in pre-clinical models of colorectal cancer.
Meeting Colorectal Cancer Head-On
Colorectal cancer (CRC) is a critical problem in global public health, with therapy-related effectivity low. In 2017 the US Food and Drug Administration (FDA) approved regorafenib, but its non-good water solubility, low oral absorption efficiency, highly necessitated doses, and the need for frequent administration with dose-related toxicity still produce in critical clinical scenarios.
To address key issue, a team of researchers from the Shanghai Institute of Materia Medica (SIMM) of Chinese Academy of Sciences proposed and developed a new strategy which combines gut-microbiome manipulation with site-specific drug targeting. The goal was to improve the pharmacokinetic attributes of regorafenib and its anti-tumor effectiveness.
Advantage 1: The Prebiotic Carrier
This is based on the employment of inulin derivative as a carrier to deliver regorafenib. The attributes of the prebiotic substance inulin make it an excellent solution for colon-targeted drug delivery.
One, inulin is resistant to gastric acid and digestive enzymes, protecting the drug payload as it passes through the upper GI. Second, inulin is exclusively degraded by the microflora in the colon which leads to site-specific drug release.
Furthermore, Ishizuka et al. showed that inulin can promote the growth of beneficial bacteria, regulate metabolism and immune homeostasis, maintain intestinal barrier function [14]. The researchers used an inulin-based nanoparticle (UIRN) to incorporate regorafenib’s prebiotic effects into a therapeutic strategy by improving drug REV-9th overall effectiveness.
Conclusion
This inulin-based drug delivery system is, therefore, a significant step forward for colorectal cancer therapies. This study suggests a novel approach to augment the anti-tumor immune response and provide clinical benefit by optimizing the pharmacokinetic attributes of regorafenib while modulating gut microbiota. Gradient-oriented, text-it out for both of us way (;This level-headed strategy could define the destiny of future treatments of colorectal cancer.
