Preparation and Characterization of Raloxifene- and Rutin-Co-loaded Chitosan Nanoparticles for the Treatment of Colon...

Colorectal cancer is a significant health concern with high incidence and mortality rates. Raloxifene (RLX) is a selective estrogen receptor modulator that blocks estrogen receptors, reducing the risk of estrogen-dependent cancer growth. Rutin (RT), a naturally occurring flavonoid found in medicinal plants, has attracted attention for its potential role in cancer prevention and treatment, including colon cancer.

In this study, the nanoparticles were prepared by the ionic gelation method. The synthesized nanoparticles were characterized by release assays and FTIR, SEM, and TEM, while their cytotoxic effects were assessed on the HT-29 colon cancer cell line.

The drug loading percentage of RLX/RT/CsNPs was found to be 84% at a 1:2 w/w ratio. SEM and TEM analyses revealed that the RLX/RT/CsNPs exhibited an average size of 57.23 nm with a spherical morphology. Thermogravimetric analysis of the nanoparticles revealed a two-stage weight loss pattern, and the drug release study showed RLX/CsNPs = 44.12%, RLX = 10.68%, and RLX/RT/CsNPs = 47.12% drug release at 24 hrs.

The IC50 value of RLX/RT/CsNPs was 23.51 ± 0.60 μM, which was significantly lower compared with the IC50 of RLX/CsNPs (IC50 = 252.20 ± 7.80 μM, p < 0.001) and RT/CsNPs (IC50 = 300.51 ± 52.05 μM, p < 0.001) against the HT-29 colon cancer cell lines.

In conclusion, we developed a new nanoparticle system combining RLX and RT showing favorable physicochemical characteristics and synergistic effects in colon cancer cell lines. The designed NPs can be used as a promising drug therapy against colon cancer.