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This study aimed to synthesize dual‐crosslinked chitosan‐alginate nanocomposites (Cs‐Alg/IO NCs) using green‐synthesized iron oxide nanoparticles (IO, Fe3O4 NPs) for drug delivery application. The NCs, formed via ionotropic gelation with sodium tripolyphosphate (TPP) and calcium chloride (CaCl2) as crosslinking agents for Cs and Alg, respectively, and further characterized for physiochemical properties. The presence of Fe3O4 NPs and 5‐Fluorouracil (5FU) increased hydrodynamic size (153.12 ± 0.57 to 207.64 ± 3.59 nm). Morphological studies revealed NC agglomeration within nanoscales. 5FU‐loaded Cs‐Alg/IO NCs (Cs‐Alg/IO 5FU NCs) exhibited superparamagnetic behavior and sustained drug release under various pH conditions. Cytotoxicity assays on colon cancer cells (HCT116 and HT‐29) and normal colon cells (CCD‐112) indicated higher cancer cell selectivity (selectivity index, SI = 1.91) in 2D models. Elevated IC50 values in 3D models were linked to lower drug loading capacity (LC) and encapsulation efficiency (EE). Overall, the study highlights the potential of dual‐crosslinked biopolymer NCs with green‐synthesized Fe3O4 NPs for developing an anticancer drug delivery system in colorectal cancer treatment. Highlights: Synthesis of 5FU‐loaded dual crosslinked Cs‐Alg/IO NCs and Cs‐Alg IPN.Physicochemical characterization of cross‐linked magnetic nanocarriers.Investigation of sustained drug release using superparamagnetic nanocarriers.Evaluation of selective cytotoxicity for Cs‐Alg/IO 5FU NCs. [ABSTRACT FROM AUTHOR]

Polysaccharide nanocrystals have great potential to be used as improved drug carriers due to their low cost, high biodegradability, and biocompatibility. This study reports the synthesis of cellulose nanocrystals (CNC) loaded with 5-fluorouracil (CNC/5FU) to evaluate their anticancer activity against colorectal cancer cells. X-ray and Fourier-transform infrared spectroscopy demonstrated that acid hydrolysis successfully degraded the amorphous cellulose to liberate the crystal regions. From transmission electron microscopy, CNC/5FU appeared as rod-like nanocrystals with an average length and width of 69.53 ± 1.14 nm and 8.13 ± 0.72 nm, respectively. The anticancer drug 5FU showed improved thermal stability after being loading onto CNC. From UV–vis spectroscopy data, the drug encapsulation efficiency in CNC/5FU was estimated to be 83.50 ± 1.52%. The drug release of CNC/5FU was higher at pH 7.4 compared to those at pH 4.2 and 1.2. From the cytotoxicity assays, CNC did not affect the viability of CCD112 colon normal cells. On the other hand, CNC/5FU exhibited anticancer effects against HCT116 and HT-29 colorectal cancer cells. The anticancer actions of CNC/5FU against HCT116 cells were then confirmed using an in vitro tumor-on-chip model and clonogenic assay. Mechanistic studies demonstrated that CNC/5FU killed the cancer cells by mainly inducing cell apoptosis and mitochondrial membrane damage. Overall, this study indicated that CNC/5FU could be a potential nanoformulation for improved drug delivery and colorectal cancer treatment. • Rod-shaped cellulose nanocrystals (CNC) were isolated from rice straw waste. • CNC indicated pH-sensitive drug release and swelling properties. • CNC showed high biocompatibility in colon normal cells. • The drug-loaded CNC significantly eliminated colorectal cancer cells using in vitro tumor-on-chip model. [ABSTRACT FROM AUTHOR]

Polysaccharide-based magnetic nanocomposites can eminently illuminate several attractive features as anticancer drug carriers. In this study, rice straw-based cellulose nanowhisker (CNW) was used as solid support for Fe 3 O 4 nanofillers to synthesize magnetic CNW. Then, cross-linked chitosan-coated magnetic CNW for 5-fluorouracil carrier abbreviated as CH/MCNW/5FU. Fourier-transform infrared, X-Ray diffraction, and X-ray photoelectron spectroscopy analysis indicated successful fabrication and multifunctional properties of the CH/MCNW/5FU nanocomposites. In addition, CH/MCNW/5FU nanocomposites showed hydrodynamic diameter and zeta potential value of 181.31 ± 3.46 nm and +23 ± 1.8 mV, respectively. Based on images of transmission electron microscopy, magnetic CNW as reinforcement was coated with chitosan to obtain almost spherical CH/MCNW/5FU nanocomposites with an average diameter of 37.16 ± 3.08. The nanocomposites indicated desired saturation magnetization and thermal stability, high drug encapsulation efficiency, and pH-dependent swelling and drug release performance. CH/MCNW/5FU nanocomposites showed potent killing effects against colorectal cancer cells in both 2D monolayer and 3D spheroid models. These findings suggest CH/MCNW as a potential carrier for anticancer drugs with high tumour-penetrating capacity. [Display omitted] • Chitosan-coated magnetic cellulose nanocrystals as 5-Fluorouracil nanocarrier (CH/MCNC/5-FU) indicated desired physiochemical properties. • CH/MCNC/5-FU showed prolonged and sustained drug release. • CH/MCNC/5-FU caused potent killing effects against colorectal cancer cells. [ABSTRACT FROM AUTHOR]

Magnetic polymer nanocomposites are inherently multifunctional and harbor assorted physiochemical actions for applications thereof as novel drug nanocarriers. Herein, Fe 3 O 4 -nanoparticles were supported on rice straw cellulose for 5-fluorouracil carrier abbreviated as MC/5-FU for potential colorectal cancer treatments. Several analyses indicated the multifunctional properties of MC/5-FU bionanocomposites. Transmission and scanning electron microscopy study demonstrated that Fe 3 O 4 nanofillers covered the cellulose matrix. The drug release from MC/5-FU was evaluated under various pH and temperature conditions, showing the maximum release at pH 7.4 and 44.2 °C. In in vitro anticancer assay, MC/5-FU exhibited enhanced selectivity and anticancer actions against 2D monolayer and 3D tumour spheroid models colorectal cancer cells. The anticancer effects of MC/5-FU with magnetic targeting and heat induction were also examined. This easily synthesized MC/5-FU indicated the potential in application as a low-cost drug formulation for colorectal cancer treatments. • Preparation of 5-fluorouracil loaded magnetic cellulose (MC/5-FU) as a low-cost and multifunctional bionanocomposites. • The release of drug from MC/5-FU increased with increase of pH and the temperature induction. • MC/5-FU improved the selectivity and anticancer activities towards 3D tumour spheroid models colorectal cancer cells. • MC/5-FU indicated negligible toxicity to the red blood cells in hemolysis assay. • The effect of magnetic targeting and heat induction on the killing of the colorectal tumour spheroid was investigated. [ABSTRACT FROM AUTHOR]

Cellulose and chitosan with remarkable biocompatibility and sophisticated physiochemical characteristics can be a new dawn to the advanced drug nano-carriers in cancer treatment. This study aims to synthesize layer-by-layer bionanocomposites from chitosan and rice straw cellulose encapsulated 5-Fluorouracil (CS-CF/5FU BNCs) using the ionic gelation method and the sodium tripolyphosphate (TPP) cross-linker. Data from X-ray and Fourier-transform infrared spectroscopy showed successful preparation of CS-CF/5FU BNCs. Based on images of scanning electron microscopy, 48.73 ± 1.52 nm was estimated for an average size of the bionanocomposites as spherical chitosan nanoparticles mostly coated rod-shaped cellulose reinforcement. 5-Fluorouracil indicated an increase in thermal stability after its encapsulation in the bionanocomposites. The drug encapsulation efficiency was found to be 86 ± 2.75%. CS-CF/5FU BNCs triggered higher drug release in a media simulating the colorectal fluid with pH 7.4 (76.82 ± 1.29%) than the gastric fluid with pH 1.2 (42.37 ± 0.43%). In in vitro cytotoxicity assays, cellulose fibers, chitosan nanoparticles and the bionanocomposites indicated biocompatibility towards CCD112 normal cells. Most promisingly, CS-CF/5FU BNCs at 250 µg/mL concentration eliminated 56.42 ± 0.41% of HCT116 cancer cells and only 8.16 ± 2.11% of CCD112 normal cells. Therefore, this study demonstrates that CS-CF/5FU BNCs can be considered as an eco-friendly and innovative nanodrug candidate for potential colorectal cancer treatment. [ABSTRACT FROM AUTHOR]

Nanoemulsions (NEs) as multi-compartmentalized systems are extensively considered as versatile drug delivery systems, due to their multifunctional and tuneable physicochemical properties. Here, water-in-oil-in-water (WOW) NEs were formulated using Juglans regia -based Fe 3 O 4 /Au-core-shell nanoparticles to encapsulate 5-Fluorouracil (5-FU) for potential colorectal cancer treatment. Response surface methodology, FTIR, TGA, TEM, DLS, VSM, UV-vis spectroscopy, and viscosity measurements were used to characterize the fabricated samples. The analysis confirmed the successful synthesis of Au, Fe 3 O 4 , and Fe 3 O 4 /Au core-shell nanoparticles with the Juglans regia (J. regia) extract as a green stabilizer and also reducing agent. The NE displayed a spherical-shape and TEM size of~30 nm. It also exhibited good colloidal stability and multifunctional features related to its components. TGA data indicated that 5-FU increased thermal stability after its loading into the nanoemulsion as a drug carrier. 5-FU release from the NE carrier presented a time-delayed behavior and higher release dosage in media at pH 4 compared to pH 7 within 48 h. When tested against colorectal-derived cell lines, 0.78 µg/mL of 5-FU-loaded Fe 3 O 4 /Au core-shell NEs showed potent anticancer activity against HCT116 cancerous cells, while exhibiting low toxicity towards CCD112 normal cells. In conclusion, the synthesized 5-FU-loaded NEs can be potently used as an anticancer drug carrier model, owing to its nano-scale size and other functionalities, which should be further studied. [ABSTRACT FROM AUTHOR]