Development and evaluation of transferrin-stabilized paclitaxel nanocrystal formulation

Area of Science:

• Nanomedicine
• Drug Delivery
• Biotechnology

Background:

• Paclitaxel is a widely used chemotherapy drug.
• Developing effective and less toxic drug delivery systems for paclitaxel is crucial for cancer therapy.
• Nanocrystal formulations can improve drug solubility and bioavailability.

Purpose of the Study:

• To prepare and evaluate a paclitaxel nanocrystal formulation stabilized by the serum protein transferrin.
• To assess the in vivo antitumor efficacy and toxicity of the paclitaxel-transferrin formulation.
• To explore the potential of non-covalently stabilized serum protein-drug nanocrystals in cancer treatment.

Main Methods:

• Paclitaxel nanocrystals were prepared using antisolvent precipitation and sonication.
• Transferrin was selected as a stabilizer after evaluating other serum proteins like albumin and immunoglobulin G.
• In vivo antitumor efficacy and toxicity were assessed in mice bearing KB cell tumors.

Main Results:

• The paclitaxel-transferrin formulation demonstrated a 45.1% tumor inhibition rate, significantly higher than paclitaxel nanosuspension (28.8%).
• While Taxol® showed higher antitumor activity (93.3% inhibition), the paclitaxel-transferrin formulation exhibited lower toxicity, evidenced by stable mouse body weight.
• The formulation was stable for at least 3 months at 4°C and contained 55-60% drug.

Conclusions:

• Transferrin-stabilized paclitaxel nanocrystals represent a promising drug delivery model for anticancer therapy.
• Non-covalent stabilization of paclitaxel nanocrystals with serum proteins offers a potential strategy to enhance efficacy while mitigating toxicity.
• Further research into serum protein-stabilized nanocrystal formulations could lead to improved cancer treatments.