article · Pharmaceutics
Apigenin is a natural plant flavonoid with anticancer properties, but its poor water solubility limits its therapeutic effectiveness. To overcome this, apigenin was encapsulated into chitosan nanoparticles and coated with albumin and folic acid to boost stability, improve bioavailability, and target tumour cells. Laboratory characterisation showed the resulting nanoparticles remained stably suspended with good drug loading and sustained release at physiological pH. In tests on HePG-2 liver cancer cells, the formulation demonstrated stronger anticancer action than pure apigenin. The treatment triggered programmed cell death by increasing p53 expression, inducing cell cycle arrest, elevating caspase-9 levels, and reducing Bcl-2 and MMP9 levels. It also enhanced antioxidant activity through improved enzyme regulation. Overall, the low-cost formulation offers improved stability over traditional carrier systems and shows promise as a potential treatment for hepatocellular carcinoma.
Natural compounds often hold strong therapeutic promise against cancer but fail in practice due to poor solubility and rapid breakdown. By packaging apigenin inside a protective, targeted nanoparticle delivery vehicle, this approach improves both its delivery and effectiveness against liver cancer cells. This demonstrates how nanotechnology can revive plant-derived molecules as practical candidates for modern cancer therapeutics.
The formulation could serve as a low-cost chemotherapeutic agent targeting hepatocellular carcinoma, offering potential interest to oncology drug developers and nanomedicine manufacturers. However, because the study was limited to in vitro laboratory testing on HePG-2 cell lines, this technology is at an early research stage and requires substantial in vivo animal testing, toxicity evaluation, and clinical validation before any market readiness can be achieved.
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Apigenin (Ap) is one of the most important natural flavonoids that has potent anticancer activity. This study was designed, for the first time, to load Ap into chitosan to improve its hydrophobicity and then it was coated with albumin-folic acid to increase its stability and bioavailability and to target cancer cells. The newly developed encapsulated Ap (Ap-CH-BSA-FANPs) was characterized and tested in vitro. The zeta potential of -17.0 mV was within the recommended range (-30 mV to +30 mV), indicating that encapsulated apigenin would not quickly settle and would be suspended. The in vitro results proved the great anticancer activity of the encapsulated apigenin on HePG-2 cells compared to pure Ap. The treated HePG-2 cells with Ap-CH-BSA-FANPs demonstrated the induction of apoptosis by increasing p53 gene expression, arresting the cell cycle, increasing caspase-9 levels, and decreasing both the MMP9 gene and <i>Bcl-2</i> protein expression levels. Moreover, the higher antioxidant activity of the encapsulated apigenin treatment was evident through increasing SOD levels and decreasing the CAT concentration. In conclusion, the Ap-CH-BSA-FANPs were easy to produce with low coast, continued drug release, good loading capacity, high solubility in physiological pH, and were more stable than the formerly Ap-loaded liposomes or PLGA. Moreover, Ap-CH-BSA-FANPs may be a promising chemotherapeutic agent in the treatment of HCC.
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DOI: 10.3390/pharmaceutics14061160
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