What question did this study set out to answer?

This study aims to develop a nanoparticle delivery system that targets colorectal cancer lesions while improving therapeutic efficacy.

July 1, 2026Journal of Nanobiotechnology0 citationsOpen Access

In situ sol-gel-sol transformation formed by sodium alginate realizes folic acid-modified chitosan nanoparticles to deliver hops β-acids for colorectal cancer therapy

XQXia QiaoNingxia Medical University JLJ T LiuUniversity of Macau JBJing BaiFirst Affiliated Hospital of Hebei Medical University

Key Points

This study aims to develop a nanoparticle delivery system that targets colorectal cancer lesions while improving therapeutic efficacy.
Designed folic acid-modified, CRC cell-targeting nanoparticles encapsulated in a sodium alginate hydrogel.
Evaluated pH-dependent release of β-acids from nanoparticles and assessed biocompatibility in vitro.
Conducted in vivo studies to evaluate toxicity and therapeutic efficacy in colorectal cancer.
The nanoparticle/hydrogel system showed cumulative release rates: pH 7.8 > pH 6.8 > pH 1.2.
In vivo studies revealed non-toxic nanoparticles that significantly inhibited colorectal cancer.
Cellular uptake was enhanced in HCT116 and HT29 cells, indicating effective targeting.

Abstract

Oral administration can deliver targeted nanoparticles directly to colorectal cancer (CRC) lesions, bypassing systemic circulation. However, orally administered nanoparticles may become physically entrapped in the small intestine, compromising therapeutic efficacy. To overcome this limitation, we designed and prepared folic acid-modified, CRC cell-targeting nanoparticles (FA/CS/TPP/β-acids) and incorporated them into a sodium alginate hydrogel (Alg/FA/CS/TPP/β-acids). The release of β-acids from the nanoparticles was pH-dependent, with cumulative release following the order: pH 7.8 > pH 6.8 > pH 1.2. The nanoparticle/hydrogel system exhibits good biocompatibility (hemolytic activity < 5%; non-toxic to NCM460 cells) and significantly enhances cellular uptake in HCT116 and HT29 cells. In vivo studies showed that the nanoparticles were non-toxic and effectively inhibited CRC. Interestingly, the hydrogel undergoes a sol-gel transition under acidic gastric conditions (pH 1.2). Upon reaching the colorectum, where the pH is higher, it undergoes a gel-sol transition. These results demonstrate that the alginate-modified hydrogel can protect the nanoparticles in the gastrointestinal environment, enabling targeted release for CRC therapy.

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