Optimization and dissolution performance of spray-dried naproxen nano-crystals

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery

Background:

• Naproxen nano-crystalline powders offer potential for enhanced drug delivery.
• Controlling particle size and physical stability is crucial for effective nano-crystallization.
• Spray-drying is a key technique for producing stable nano-crystalline powders.

Purpose of the Study:

• To investigate the in vitro dissolution of different sized spray-dried naproxen nano-crystalline powders.
• To optimize nano-crystalline suspensions using a Design of Experiments (DoE) approach.
• To characterize the physical properties and dissolution performance of the resulting powders.

Main Methods:

• Formulation and optimization of nano-crystalline suspensions via wet milling.
• Spray-drying of optimized suspensions with auxiliary excipients (trehalose, lactose).
• Characterization using particle size analysis, Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD).
• In vitro dissolution testing using a modified USP Apparatus II with a dialysis sac method.

Main Results:

• Nano-crystalline suspension size was influenced by drug concentration and milling intensity.
• HPMC E15 formulations yielded better spray-dried powder recovery than Tween 80.
• Trehalose was effective in producing non-aggregating nano-crystalline powders.
• No polymorphic changes were observed during processing.
• Obtained size-dependent in vitro dissolution profiles for the naproxen nano-crystalline powders.

Conclusions:

• Optimized spray-dried naproxen nano-crystalline powders exhibit size-dependent dissolution.
• The study successfully developed a method for producing stable nano-crystalline powders with tunable dissolution characteristics.
• This approach holds promise for improving naproxen bioavailability and therapeutic efficacy.