Physicochemical characterization and dissolution properties of meloxicam-gelucire 50/13 binary systems

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Meloxicam (MX) is a poorly soluble non-steroidal anti-inflammatory drug (NSAID).
• Improving the biopharmaceutical and pharmacological properties of MX is crucial for effective treatment.
• Solid dispersions offer a promising approach to enhance the solubility and bioavailability of poorly soluble drugs.

Purpose of the Study:

• To prepare a solid dispersion of Meloxicam (MX) using Gelucire 50/13 via spray drying.
• To characterize the solid dispersion and evaluate its dissolution rate and anti-inflammatory activity.
• To assess the suitability of spray drying for enhancing MX properties.

Main Methods:

• Spray drying was employed to prepare Meloxicam-Gelucire 50/13 solid dispersions.
• Scanning electron microscopy (SEM) was used for particle morphology analysis.
• Differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) were utilized to confirm the amorphous state of MX.
• In vitro dissolution tests at pH 7.4 and in vivo anti-inflammatory activity assessment (rat paw edema model) were performed.

Main Results:

• Spherical microparticles with smooth surfaces were successfully prepared by spray drying.
• Meloxicam transformed from crystalline to amorphous state within the solid dispersion, evidenced by DSC and PXRD.
• Dissolution rate of encapsulated MX was 2.5-fold higher than physical mixture and 4-fold higher than MX alone.
• Microparticles at a 1:4 drug/Gelucire ratio showed 4-fold higher anti-inflammatory activity compared to MX alone.

Conclusions:

• Spray drying is an effective technique for producing Meloxicam-Gelucire 50/13 solid dispersions.
• The amorphous solid dispersion significantly enhances the dissolution rate and anti-inflammatory efficacy of Meloxicam.
• This approach offers a viable strategy for improving the therapeutic potential of poorly soluble NSAIDs.