Development and characterization of solid dispersion-microsphere controlled release system for poorly water-soluble...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Poorly soluble drugs pose challenges for effective therapeutic delivery.
• Conventional formulations often result in rapid drug release and limited efficacy.
• Developing advanced drug delivery systems is crucial for improving drug performance.

Purpose of the Study:

• To enhance the solubility and prolong the release of a poorly soluble drug, Flurbiprofen (FBP).
• To develop a controlled-release formulation by combining solid dispersion and microsphere technologies.
• To evaluate the in vitro and in vivo performance of the developed formulation.

Main Methods:

• Solid dispersions were prepared using urea and mannitol via fusion.
• Microspheres were fabricated using Eudragit L-100 and Eudragit RS PO via solvent evaporation.
• Controlled-release formulations were created by blending optimized solid dispersion and microspheres.
• Formulations were characterized for yield, drug content, morphology (SEM), in vitro release, and in vivo anti-inflammatory activity.

Main Results:

• SEM confirmed spherical microspheres with particle sizes between 73.5-85.4 μm.
• The optimal formulation (solid dispersion:microspheres at 1:0.5) achieved sustained FBP release for up to 10 hours.
• Drug release followed zero-order kinetics, indicating diffusion-controlled release.
• The formulation demonstrated significant inhibition of rat paw edema for 16 hours.

Conclusions:

• A binary mixture of solid dispersion and microspheres effectively improves solubility and prolongs drug release.
• This approach offers a promising strategy for the controlled delivery of poorly soluble drugs with pH-dependent solubility.
• The developed formulation is suitable for controlled delivery of Flurbiprofen, enhancing its therapeutic potential.