Physical characterization and dissolution performance assessment of Etravirine solid dispersions prepared by spray...

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Etravirine (ETV) exhibits poor aqueous solubility, limiting its oral bioavailability and therapeutic efficacy.
• Enhancing Etravirine's solubility and dissolution rate is crucial for improving its pharmacokinetic profile.
• Solid dispersion technology offers a promising approach to overcome solubility challenges in poorly soluble drugs.

Purpose of the Study:

• To prepare solid dispersions (SD) of Etravirine using spray drying.
• To enhance the aqueous solubility and dissolution rate of Etravirine.
• To characterize the physical properties and evaluate the in vitro drug release of Etravirine SDs.

Main Methods:

• Etravirine solid dispersions were prepared using spray drying with Copovidone and Povidone-Copovidone.
• Characterization involved Scanning Electron Microscopy (SEM), X-Ray Diffractometry (PXRD), FTIR, and Differential Scanning Calorimetry (DSC).
• In vitro drug release studies were conducted in three different pH media, analyzed using the Weibull model.

Main Results:

• Spray drying converted crystalline Etravirine to an amorphous form within the solid dispersions.
• Solid dispersions exhibited significantly enhanced equilibrium solubility compared to physical mixtures and intact Etravirine.
• Drug release kinetics followed the Weibull mathematical model, with improved Mean Dissolution Time (MDT) and Dissolution Efficiency (DE %).

Conclusions:

• Spray drying is an effective technique for preparing amorphous solid dispersions of Etravirine.
• The prepared solid dispersions demonstrate improved solubility and dissolution profiles, indicating enhanced bioavailability.
• The Weibull model effectively describes the drug release kinetics, providing valuable insights for formulation development.