Abstract
In spite of the major advantages that the liquisolid technology offers, particularly in tackling poor bioavailability of poorly water-soluble drugs (i.e., BCS Class II drugs), there are a few critical drawbacks. The inability of a high liquid load factor, poor flowability, poor compactibility, and an inability to produce a high dose dosage form of a reasonable size for swallowing are major hurdles, hampering this technology from being commercially feasible. An attempt was therefore made to overcome these drawbacks whilst maintaining the liquisolid inherent advantages. This resulted in the emerging next generation of oral dosage forms called the liqui-pellet. All formulations were incorporated into capsules as the final product. Solubility studies of naproxen were conducted in different liquid vehicles, namely polyethylene glycol 200, propylene glycol, Tween 80, Labrafil, Labrasol, and Kolliphor EL. The scanning electron microscopy studies indicated that the liquid vehicle tends to reduce the surface roughness of the pellet. X-ray powder diffraction (XRPD) indicated no significant differences in the crystalline structure or amorphous content between the physical mixture and the liqui-pellet formulation. This was due to the presence of a high concentration of amorphous Avicel in the formulation which overshadowed the crystalline structure of naproxen in the physical mixtures. Flowability and dissolution tests confirmed that this next-generation oral dosage form has excellent flowability, whilst maintaining the typical liquisolid enhanced drug release performance in comparison to its physical mixture counterpart. The liqui-pellet also had a high liquid load factor of 1, where ~ 29% of the total mass was the liquid vehicle. This shows that a high liquid load factor can be achieved in a liqui-pellet without compromising flowability. Overall, the results showed that the poor flowability of a liquisolid formulation could be overcomed with the liqui-pellet, which is believed to be a major advancement into the commercial feasibility of the liquisolid concept.
Highlights
Liqui-pellet is an emerging novel oral dosage form, which improves the bioavailability of poorly water-soluble drugs via increasing drug release rate in the GIT
The results showed that the poor flowability of a liquisolid formulation could be overcomed with the liqui-pellet, which is believed to be a major advancement into the commercial feasibility of the liquisolid concept
It is worth pointing out that around 60% of drugs in the market are poorly soluble in gastrointestinal fluids, which is based on biopharmaceutical classification system (BCS), and around 40% of drugs in development are identified as poorly water soluble [2,3]
Summary
Liqui-pellet is an emerging novel oral dosage form, which improves the bioavailability of poorly water-soluble drugs via increasing drug release rate in the GIT. Liqui-pellet stems from combining liquisolid concept with pelletization technology. The liquipellet cannot be described as a liquisolid system because it is not necessarily in powder form and the admixture is not necessarily free-flowing, but rather a cohesive wet mass. The purpose of entitling the new dosage form as liqui-pellet is to emphasize the high liquid load factor or high amount of liquid vehicle it is capable of containing. This implies that a high amount of liquid medication can be
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