Abstract
Colorectal cancer (CRC) is the third highest major cause of morbidity and mortality worldwide. Hence, many strategies and approaches have been widely developed for cancer treatment. This work prepared and evaluated the antitumor activity of 5-Fluorouracil (5-Fu) loaded chromium nanoparticles (5-FuCrNPs). The green biosynthesis approach using Harpullia (H) pendula aqueous extract was used for CrNPs preparation, which was further loaded with 5-Fu. The prepared NPs were characterized for morphology using scanning and transmission electron microscopes (SEM and TEM). The results revealed the formation of uniform, mono-dispersive, and highly stable CrNPs with a mean size of 23 nm. Encapsulation of 5-Fu over CrNPs, with a higher drug loading efficiency, was successful with a mean size of 29 nm being produced. In addition, Fourier transform infrared (FTIR) and X-ray diffraction pattern (XRD) were also used for the investigation. The drug 5-Fu was adsorbed on the surface of biosynthesized CrNPs in order to overcome its clinical resistance and increase its activity against CRC cells. Box–Behnken Design (BBD) and response surface methodology (RSM) were used to characterize and optimize the formulation factors (5-Fu concentration, CrNP weight, and temperature). Furthermore, the antitumor activity of the prepared 5-FuCrNPs was tested against CRC cells (CACO-2). This in vitro antitumor study demonstrated that 5-Fu-loaded CrNPs markedly decreased the IC50 of 5-Fu and exerted more cytotoxicity at nearly all concentrations than 5-Fu alone. In conclusion, 5-FuCrNPs is a promising drug delivery system for the effective treatment of CRC.
Highlights
Colorectal cancer (CRC) is the third highest major cause of morbidity and mortality worldwide [1]
H. pendularutin, plant, previously have been isolated andbeen characterized from the H. pendula plant, viincluding rutin, vitexin, isovitexin, orientin, quercetin, and kaempferol quercetin-3-O-βD
Members of apiofuranosyl (1′′′→2′′)-β-galactopyranoside [31,33]. Members of this family have been widely studied for their antioxidant, anti-inflammatory, insecticidal, this family have been widely studied for their antioxidant, anti-inflammatory, insecticidal, and anti-diabetic properties [45,46,47,48]
Summary
Colorectal cancer (CRC) is the third highest major cause of morbidity and mortality worldwide [1]. Many strategies have been developed for cancer treatment, including. Pharmaceutics 2021, 13, 226 surgery, chemotherapy, and radiation [2,3,4]. Despite advances in treatment strategies, resistance to chemotherapy represents a challenge in the management of the incurable metastatic disease [5]. The drug 5-Fluorouracil (5-Fu) is a well-known chemotherapeutic agent, used as a first-line treatment for CRC [6,7]. The acquired drug resistance, short half-life of 10–20 min, and harmful side effects on the bone marrow and gastrointestinal tract (GIT), remain among the limitations of its clinical use [9,10]. Considerable attention has been paid to using 5-Fu-based mix regimens and 5-Fu pro-drugs to conquer the clinical opposition and increase its anti-tumor activity [6]
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