Pantoprazole Sodium Loaded Microballoons for the Systemic Approach: In Vitro and In Vivo Evaluation

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Gastroenterology

Background:

• Floating and pulsatile drug delivery systems face challenges with variable gastric transit times, impacting drug bioavailability.
• Pantoprazole Sodium (PAN) requires optimized delivery to enhance its therapeutic efficacy and patient compliance.

Purpose of the Study:

• To develop Pantoprazole Sodium (PAN) microballoons for prolonged gastric residence time.
• To enhance the bioavailability and anti-ulcer activity of Pantoprazole Sodium through microballoon formulation.

Main Methods:

• Microballoons were prepared using Eudragit®L100 via emulsion solvent diffusion (non-effervescent approach).
• In vitro studies, in vivo evaluation (ethanol-induced ulceration), SEM, DSC, and optimization using Design Expert® software were conducted.

Main Results:

• Optimized microballoons (LRS-O) showed increased yield, buoyancy, encapsulation efficacy, and swelling.
• Particles ranged from 80-100 µm with zero-order release, porous spherical structures, and amorphous drug encapsulation.
• The optimized formulation exhibited significant anti-ulcer activity (ulcer index 0.20±0.05, protection 97.43%).

Conclusions:

• Developed Pantoprazole Sodium microballoons offer prolonged gastric residence and enhanced bioavailability.
• The pH-dependent microballoon system provides an efficient dosage regimen with improved patient compliance.