Exploring the Dissolution, Solid-state Properties, and Long-term Storage Stability of Cryoprotectant-free...

Area of Science:

• Pharmaceutical Nanotechnology
• Drug Delivery Systems
• Materials Science

Background:

• Fenbendazole, an antiparasitic, shows potential in cancer therapy but suffers from poor solubility.
• Hydrophobicity limits fenbendazole's dissolution rate and absorption, hindering its therapeutic efficacy.
• Nanotechnology offers a strategy to overcome fenbendazole's solubility challenges.

Purpose of the Study:

• To improve fenbendazole's solubility and dissolution performance using a nanotechnological approach.
• To formulate fenbendazole nanoparticles stabilized by poloxamers.
• To evaluate the physicochemical properties and stability of the fenbendazole nanosystems.

Main Methods:

• Fenbendazole nanoparticles were prepared via lyophilization using various poloxamers as stabilizers.
• Solid-state characterization included X-ray diffractometry, differential scanning calorimetry, and infrared spectroscopy.
• Solubility, dissolution rate, particle size, polydispersity, and long-term stability were assessed.

Main Results:

• Nanoparticles exhibited submicron sizes (< 340 nm) with low polydispersity, influenced by the poloxamer stabilizer.
• Physicochemical analysis revealed significant drug amorphization, enhancing solubility and dissolution.
• Dissolution rates of both fresh and aged nanoparticles were markedly higher than the raw drug.
• Poloxamer 407 stabilized nanoparticles showed good particle size stability over three years.
• Some recrystallization occurred in nanoparticles stabilized by P188, P237, and P407 during long-term storage.

Conclusions:

• Poloxamers effectively stabilize fenbendazole nanoparticles, significantly improving drug dissolution.
• Amorphization of fenbendazole within the nanosystems is key to enhanced solubility and release.
• Poloxamer 407 demonstrates superior performance in maintaining nanoparticle stability over time.
• These findings highlight the potential of poloxamer-based nanosystems for improved fenbendazole delivery.