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Preparation and Characterization of SDF-1α-Chitosan-Dextran Sulfate Nanoparticles
Published on: January 22, 2015
Development and characterization of engineered gingerol loaded chitosan nanoparticles for targeting colon cancer,
Mahmoud A Abdelaziz1, Adel I Alalawy2, Mohamed Sobhi1
1Department of Chemistry, Faculty of Science, University of Tabuk, P.O. Box 741, Tabuk 71491, Saudi Arabia.
Abstract:
This study presents the development of a multifunctional nanotherapeutic platform based on gingerol (GN) loaded chitosan nanoparticles (GN@CsNPs), designed to simultaneously target colorectal cancer, combat enteric bacterial infections, and alleviate oxidative stress. The nanoformulation system demonstrated a high sustained release profile, releasing 60 % of GN within 8 h and achieving 98.5 % cumulative release under acidic conditions (pH 4.2) over 72 h, supporting targeted colonic delivery. Cytotoxicity assays against HCT-116 colon cancer cells revealed strong dose-dependent effects, with an IC50 of 73.2 μg/mL and up to 93.4 % inhibition of cell viability at 250 μg/mL. Antibacterial evaluations confirmed broad-spectrum efficacy, with inhibition zones of 19 ± 0.36 mm (E. coli) and 21 ± 0.82 mm (Salmonella enterica), MIC values ranging from 150 to 300 μg/mL, and MBC values up to 350 μg/mL. Time-kill studies demonstrated complete bacterial eradication within 15-30 min at 2 × MIC. Antioxidant analysis revealed robust free radical scavenging (83.0 % at 1000 μg/mL), with an IC50 of 30.9 μg/mL, significantly outperforming unloaded CsNPs. Molecular docking studies supported the dual functionality of GN, showing high binding affinity to both mTOR (-6.1 kcal/mol) and gtfB (-6.1 kcal/mol), implicating its roles in anticancer and antimicrobial mechanisms. In conclusion, the results position GN@CsNPs as a promising bio-based nanotherapeutic for integrated management of colorectal cancer, microbial infections, and oxidative stress-related conditions.
Insights
This study developed gingerol-loaded chitosan nanoparticles (GN@CsNPs) for colorectal cancer, bacterial infections, and oxidative stress. The nanotherapeutic showed significant anticancer, broad-spectrum antibacterial, and antioxidant effects, offering integrated treatment potential.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Pharmacology
Background:
- Colorectal cancer (CRC) poses a significant health burden, often accompanied by bacterial infections and oxidative stress.
- Current treatments have limitations, necessitating novel therapeutic strategies for integrated management.
Purpose of the Study:
- To develop a multifunctional nanotherapeutic platform using gingerol (GN) loaded chitosan nanoparticles (GN@CsNPs).
- To evaluate the efficacy of GN@CsNPs in targeting colorectal cancer, combating enteric bacterial infections, and alleviating oxidative stress.
Main Methods:
- Nanoformulation of GN@CsNPs with sustained release properties under acidic conditions (pH 4.2).
- In vitro cytotoxicity assays against HCT-116 colon cancer cells.
- Antibacterial evaluations including inhibition zones, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC).
- Antioxidant activity assessment via free radical scavenging assays.
- Molecular docking studies to elucidate anticancer and antimicrobial mechanisms.
Main Results:
- GN@CsNPs exhibited a sustained release profile, with 98.5% cumulative release at pH 4.2 over 72 hours.
- Significant dose-dependent cytotoxicity against HCT-116 cells (IC50 = 73.2 μg/mL) and up to 93.4% inhibition.
- Broad-spectrum antibacterial activity against E. coli and Salmonella enterica (MICs 150-300 μg/mL, MBCs up to 350 μg/mL).
- Potent antioxidant capacity with 83.0% free radical scavenging at 1000 μg/mL (IC50 = 30.9 μg/mL).
- Molecular docking revealed high binding affinity of GN to mTOR and gtfB, supporting its dual functionality.
Conclusions:
- GN@CsNPs represent a promising bio-based nanotherapeutic platform for integrated management.
- The developed system effectively targets colorectal cancer, combats bacterial infections, and mitigates oxidative stress.
- Further research is warranted to explore the in vivo potential of GN@CsNPs for clinical applications.
