Design, statistical optimisation, characterisation and pharmacodynamic studies on Pioglitazone hydrochloride floating...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Pioglitazone HCl is a key antidiabetic agent.
• Controlled release formulations aim to improve therapeutic efficacy and patient compliance.
• Floating drug delivery systems offer prolonged gastric residence time.

Purpose of the Study:

• To develop and characterize Pioglitazone HCl-loaded floating microparticles for controlled release.
• To evaluate the drug-excipient compatibility.
• To perform pharmacodynamic studies to assess in vivo efficacy.

Main Methods:

• Solvent evaporation technique was used for microparticle preparation.
• A 2(2) factorial design optimized drug:polymer ratios and Eudragit RS 100:RL 100 proportions.
• Fourier Transform Infrared (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), Scanning Electron Microscopy (SEM), buoyancy, and in vivo pharmacodynamic studies were conducted.

Main Results:

• FTIR and DSC confirmed no drug-excipient interactions.
• Factorial design successfully predicted and actualized drug release and entrapment efficiencies.
• SEM revealed spherical microparticles with reduced drug crystallinity; buoyancy studies showed 12-hour floating capability.
• Pharmacodynamic studies in rabbits demonstrated significant reduction in blood glucose levels.

Conclusions:

• Floating microparticles of Pioglitazone HCl were successfully developed using a factorial design approach.
• The formulation exhibited controlled release characteristics and effective in vivo glucose-lowering activity.
• This study highlights the potential of floating microparticles for enhanced Pioglitazone HCl therapy.