Improved Dissolution and Oral Bioavailability of Celecoxib by a Dry Elixir System

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Medicinal Chemistry

Background:

• Poorly water-soluble drugs often exhibit limited oral bioavailability.
• Dry elixir (DE) systems are effective for improving drug solubility and bioavailability.
• Celecoxib is a widely used nonsteroidal anti-inflammatory drug with poor water solubility.

Purpose of the Study:

• To develop and evaluate a dry elixir (DE) system for celecoxib.
• To enhance the dissolution rate and oral bioavailability of celecoxib.
• To investigate the characteristics of celecoxib-loaded DEs.

Main Methods:

• Celecoxib-loaded DEs were prepared using a spray-drying method.
• Characterization included morphology, drug/ethanol content, drug crystallinity, dissolution rate, and oral bioavailability studies.
• Spray-drying conditions were controlled to modulate ethanol and drug content.

Main Results:

• DEs exhibited a nano-structured matrix, amorphous state, and encapsulated ethanol, leading to enhanced dissolution.
• Dissolution rates of celecoxib from DEs were significantly higher than celecoxib powder.
• In vivo studies in rats showed markedly greater blood concentrations of celecoxib from DE formulations compared to celecoxib powder and a commercial product.

Conclusions:

• The developed DE system is a viable solid dosage form for improving celecoxib's solubility, dissolution, and oral bioavailability.
• Spray-drying offers controllable parameters for optimizing DE formulation characteristics.
• This approach holds promise for enhancing the therapeutic efficacy of poorly soluble drugs like celecoxib.