Fisetin-loaded nanocochleates: formulation, characterisation, in vitro anticancer testing, bioavailability and...

Area of Science:

• Nanotechnology
• Drug Delivery Systems
• Cancer Therapeutics

Background:

• Fisetin, a natural flavonoid, exhibits anticancer properties but faces challenges in administration due to poor solubility and metabolism.
• Effective, controlled-release, and safe fisetin formulations are crucial for advancing cancer treatment.

Purpose of the Study:

• To develop and evaluate fisetin-loaded nanocochleates to enhance fisetin's therapeutic efficacy.
• To improve the bioavailability and anticancer activity of fisetin through nanocochleate formulation.

Main Methods:

• Fisetin-loaded liposomal vesicles were converted into nanocochleates using Ca(2+) ions.
• Characterization included physicochemical properties, in vitro anticancer activity, haemolysis, pharmacokinetics, and tissue distribution studies in mice.

Main Results:

• Nanocochleates with a particle size of 275 ± 4 nm and 84.31 ± 2.52% encapsulation efficiency were successfully prepared.
• Fisetin nanocochleates demonstrated sustained release, improved in vitro anticancer activity by 1.3-fold against MCF-7 cells, and a 141-fold increase in relative bioavailability.
• The formulation exhibited safety with low tissue distribution.

Conclusions:

• The developed fisetin nanocochleates significantly enhanced anticancer efficacy, bioavailability, and safety.
• Nanocochleate technology offers a promising approach for the clinical administration of fisetin for cancer treatment.