In a study published in Advanced Functional Materials, a research team from the Shanghai Institute of Materia Medica (SIMM) of the Chinese Academy of Sciences developed an oral molecular targeted drug delivery system based on an inulin derivative, which combines gut microbiota modulation with precise drug delivery, enhancing colorectal cancer (CRC) therapy.

Regorafenib (REG), a small-molecule multi-pathway protein kinase inhibitor, was approved by U.S. Food and Drug Administration in 2017 to treat metastatic CRC. Due to its poor water solubility and low oral absorption efficiency, high doses and frequent administration are required to maintain effective intratumoral drug concentrations, which can lead to dose-related toxicity. Therefore, it is important to develop a drug delivery system that improves the pharmacokinetic properties and tumor targeting of REG.

Gut microbiota has been shown to affect the development of CRC. Both regulating gut microbiota and improving intestinal environment can serve as complementary approaches to enhance CRC therapy.

Inulin, a kind of prebiotic material, promotes the proliferation of beneficial bacteria, regulates metabolism, maintains immune balance, and protects the intestinal barrier. It is resistant to gastric acid and digestive enzymes, while is only degraded by microorganisms in the colon. These properties make inulin a potential carrier material for colon-targeting oral drug delivery.

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