A Novel Application of an Effervescent Agent in Naproxen Liqui-Pellets for Enhanced Drug Release

Liqui-Pellet formulations have been introduced as a technology to improve the dissolution rate of poorly water-soluble drugs. This study aimed to incorporate sodium bicarbonate (NaHCO 3 ) into the Liqui-Pellet formulation to explore the potential impact on the drug release rate. Naproxen Liqui-Pellet formulations containing 5%, 12%, 22%, 32%, and 42% w/w of NaHCO 3 were successfully produced and their physicochemical properties were investigated and compared with a physical mixture pellet formulation. Incorporation of such a large amount of functional excipient is impossible or near impossible in the classical liquisolid formulation due to weight and size limitations, particularly for high-dose drugs. The results showed that NaHCO 3 is an effective functional excipient to enhance the drug dissolution rate. The Liqui-Pellet formulation with 42% w/w NaHCO 3 released 76.4% of drug after 2 hours at pH 1.2, which was 14 times faster than the physical mixture pellet (5.5% drug release in 2 h). In general, a faster dissolution rate was observed with increasing NaHCO 3 concentration; however, there was a limit to this effect. Above a certain limit, the influence of NaHCO 3 on the dissolution rate lessened. The flowability test showed that all formulations have good to excellent flowability. Overall, this study demonstrates the flexibility of Liqui-Pellets in terms of formulation design, which in turn further supports the potential of Liqui-Pellets as the next generation oral dosage form.