Optimization, formulation, and characterization of multiflavonoids-loaded flavanosome by bulk or sequential...

Area of Science:

• Nanotechnology and Drug Delivery
• Phytochemistry and Natural Products

Background:

• Flavonoids possess significant therapeutic potential but often suffer from poor bioavailability.
• Developing effective delivery systems for multiple flavonoids is crucial for enhanced therapeutic outcomes.

Purpose of the Study:

• To adapt and optimize a sequential loading technique for creating a single phytosome encapsulating multiple flavonoids (quercetin, kaempferol, apigenin).
• To characterize the synthesized multi-flavonoid phytosome (flavonosome) and evaluate its antioxidant and cytotoxic properties.

Main Methods:

• Synthesis of quercetin, kaempferol, and apigenin loaded phosphatidylcholine phytosomes (flavonosomes) using four methods: bulk and sequential co-sonication, and bulk and sequential co-loading.
• Characterization of flavonosomes based on size, charge, polydispersity index, morphology, and drug-carrier interaction.
• Evaluation of antioxidant activity via DPPH assay and cytotoxicity against HepaRG cells using MTT assay.

Main Results:

• The sequential loading technique (M4) was optimized, yielding flavonosomes with an average diameter of 375.93±33.61 nm and zeta potential of -39.07±3.55 mV.
• Entrapment efficiency exceeded 98% for all flavonoids, with drug-loading capacities of 31.63%±0.17% (Q), 34.51%±2.07% (K), and 31.79%±0.01% (A).
• The synthesized flavonosomes exhibited significant antioxidant potential and no toxicity to HepaRG cells, with >85% cell viability at 200 µg/mL.

Conclusions:

• Sequential loading is an effective method for developing multi-flavonoid phytosomes (flavonosomes) with excellent encapsulation and loading efficiencies.
• The developed QKA-phosphatidylcholine flavonosome is a safe and promising nanodrug delivery system for sustained antioxidant, hepatoprotective, and hepatosupplement activities.