Abstract
Purpose: Various floating and pulsatile drug delivery systems suffer from variations in the gastric transit time affecting the bioavailability of drugs. The objective of the study was to develop Pantoprazole Sodium (PAN) microballoons that may prolong the gastric residence time and could enhance the drug bioavailability.Methods: Microballoons were prepared using Eudragit®L100 by adopting emulsion solvent diffusion method with non-effervescent approach, in vitro studies were performed and the in vivo evaluation was carried out employing ethanol induced ulceration method. Optimization and validation were carried out through Design Expert® software.Results: The results demonstrate an increase in percentage yield, buoyancy, encapsulation efficacy and swelling. Particles were in the size range 80-100 µm following zero order release pattern. SEM study revealed their rough surface with spherical shape, internal cavity and porous walls. DSC thermo gram confirms the encapsulation of drug in amorphous form. Significant anti ulcer activity was observed for the prepared microballoons. The calculated ulcer index and protection were 0.20±0.05 and 97.43 % respectively for LRS-O (optimized formulation).Conclusion: This kind of pH dependent drug delivery may provide an efficient dosage regimen with enhanced patient compliance.
Highlights
Pantoprazole Sodium (PAN) has high solubility and high permeability so it is a difficult task to restore its efficacy
Microballoons were prepared using Eudragit®L100 by adopting emulsion solvent diffusion method with non-effervescent approach, in vitro studies were performed and the in vivo evaluation was carried out employing ethanol induced ulceration method
The results demonstrate an increase in percentage yield, buoyancy, encapsulation efficacy and swelling
Summary
Pantoprazole Sodium (PAN) has high solubility and high permeability so it is a difficult task to restore its efficacy. Due to its low bioavailability (77%) and short half-life (1 h) its administration is preferred through intravenous (IV) route but for the non-invasive therapy it is given through oral route as multiple unit dosage form such as floating microspheres that efficiently reduces the dosing frequency.[1] In previous reported works it has been formulated as gastro-resistant multiple unit systems by emulsion solvent diffusion and spray-drying methods using Eudragit®S100.2 Micro particles formulated through emulsion solvent diffusion method were larger in size and were able to stabilize 61% of PAN content after acid exposure. In our study microballoons intended for extended release were prepared by non-effervescent technique using magnesium stearate, Eudragit®L100, Eudragit®RS100 and analyzed simultaneously
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