Abstract

AimLiqui-Pellet is potentially an emerging next-generation oral pill, which has shown promising results with unique advantages as well as displaying potential for commercial feasibility. Since Liqui-Pellet technology is still in its infancy, it is important to explore the parameters that can affect its performance, particularly the drug release rate. Therefore, the aim of this study is to investigate thoroughly the effect of Avicel PH101 (carrier) and Aerosil 300 (coating material) ratio (R-value) in Liqui-Pellet.MethodsKey parameter for Liqui-Pellet formulation in this study was the ratio of carrier and coating material. Tests were carried out to assess the physicochemical properties of different formulations. This involved looking into particle size, robustness, flowability, solid-state and drug release profile. The morphology of Liqui-Pellet was investigated by SEM.ResultsIt is found that R-value does not have a major effect on the success of Liqui-Pellet production. However, R-value does seem to have an effect on Liqui-Pellet size at a certain water content level and a slight effect on the drug release rate. A decrease in Avicel PH101 concentration and an increase in Aerosil 300 concentration in Liqui-Pellet formulations can reduce Liqui-Pellet size and slightly increase drug release rate by 9% after 2 h. The data shows Liqui-Pellet is resistant to friability, able to achieve exceptional flow property and have smooth surfaces, which is critical for applying coatings technology. Such properties are ideal in terms of commercial manufacturing. The XRPD and DSC both show the reduction in formulation crystallinity, which is expected in Liqui-Pellet formulation as a result of solubility of the drug in the co-solvent used in the preparation of Liqui-Pellets.ConclusionOverall it seems that R-value can affect Liqui-Pellet drug release rate and size but not on the production success rate.Graphical abstract

Highlights

  • Liqui-Pellet is an emerging novel oral dosage form, which focuses on tackling the challenges of developing future oral drug delivery system

  • The X-ray powder diffraction (XRPD) and Differential scanning calorimetry (DSC) both show the reduction in formulation crystallinity, which is expected in Liqui-Pellet formulation as a result of solubility of the drug in the co-solvent used in the preparation of Liqui-Pellets

  • Overall it seems that R-value can affect Liqui-Pellet drug release rate and size but not on the production success rate

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Summary

Introduction

Liqui-Pellet is an emerging novel oral dosage form, which focuses on tackling the challenges of developing future oral drug delivery system. Enhancement of the bioavailability of these API can potentially reduce adverse drug effects by potentially lowering dosage strength. It can potentially bring more viable API to the market through achieving acceptable bioavailability that would otherwise have not been acceptable. Liqui-Pellet is capable of enhancing the drug release rate whilst achieving excellent flow properties and high load factor unlike the classical liquisolid compact [1,2,3]. This makes the generation Liqui-Pellet formulation highly commercially feasible, unlike in the classical liquisolid technology. It is postulated that the enhanced drug release rate is due to an increase in surface area available for dissolution, increased solubility of the drug and improved wettability of drug particles [5, 6]

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