Determining the Best Poloxamer Carrier for Thiocolchicoside Solid Dispersions

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Thiocolchicoside (TCS) is a muscle relaxant with limited solubility, posing challenges for effective drug delivery.
• Solid dispersions (SDs) offer a promising approach to enhance the solubility and bioavailability of poorly soluble drugs like TCS.

Purpose of the Study:

• To identify the most effective poloxamer carrier for creating solid dispersions of thiocolchicoside (TCS).
• To evaluate the impact of different poloxamer types and ratios on TCS solubility and release characteristics.

Main Methods:

• Compatibility of TCS with various poloxamers (108, 188, 237, 338, 407) was assessed using differential scanning calorimetry and fourier transform infrared spectroscopy.
• Solid dispersions (SDs) were prepared using a microwave fusion method at different TCS:poloxamer ratios (1:1 to 1:6) and characterized for physicochemical properties and drug release.
• Drug release kinetics were analyzed using established models to understand the release mechanisms from the SD formulations.

Main Results:

• Thiocolchicoside (TCS) demonstrated good compatibility with all tested poloxamer carriers.
• The prepared solid dispersion formulations exhibited favorable physicochemical properties and drug release profiles.
• First-order release kinetics were observed for TCS from the optimized SD formulations.

Conclusions:

• Poloxamer-188 was identified as the superior carrier for thiocolchicoside (TCS) solid dispersions.
• The use of poloxamer-188 significantly improved both the solubility and the in vitro release rate of TCS.
• This study provides valuable insights for developing enhanced oral dosage forms of thiocolchicoside using poloxamer-based solid dispersions.