Spray-Dried Polymeric Microspheres for Lipophilic Drugs: Formulation Design, Physicochemical Characterization, and In...

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Aqueous methods for lipophilic drug microsphere formulation, including spray drying, present formulation challenges.
• Developing effective microsphere formulations requires careful consideration of process parameters and polymer selection.

Purpose of the Study:

• To evaluate the impact of process parameters and polymer selection on lipophilic drug microsphere production using aqueous spray drying.
• To optimize parameters for enhanced yield and encapsulation efficiency in microsphere formulations.

Main Methods:

• Lipophilic drug-loaded microspheres were prepared using Agave inulin, guar gum, hydroxypropyl methylcellulose, and Eudragit® S100 via aqueous spray drying.
• A 2^3 factorial design was employed to analyze the effects of process parameters on yield and encapsulation efficiency.
• Microsphere morphology and drug release profiles were characterized.

Main Results:

• Inlet temperature, feed flow, and polymer percentage significantly influenced guar gum microsphere yield and inulin microsphere encapsulation efficiency.
• Inulin and guar gum microspheres achieved the highest yield (75.41%) and encapsulation efficiency (100%), respectively.
• Guar gum microspheres exhibited optimal morphology, while Eudragit® S100 lost its delayed release property in the aqueous method.

Conclusions:

• Optimizing spray drying parameters (inlet temperature, feed flow) and polymer type/percentage is crucial for controlling microsphere development.
• The study demonstrates the potential of specific polymers like inulin and guar gum for improved lipophilic drug microsphere production.
• Aqueous spray drying can be optimized for better yield and encapsulation, though challenges remain for controlled release with certain polymers.