Abstract
The present study describes the use of two taste-masking polymers to fabricate a formulation of chlorpheniramine maleate for paediatric administration. Co-axial electrospinning was utilized to create layered nanofibres; the two polymers, Eudragit® E PO and Kollicoat® Smartseal, were alternated between the core and the shell of the system in order to identify the optimum taste-masked formulation. The drug was loaded in the core on all occasions. It was found that the formulation with Kollicoat® Smartseal in the core with the drug, and Eudragit® E PO in the shell showed the most effective taste-masking compared to the other formulations. These fibres were in the nano-range and had smooth morphology as verified by scanning electron microscopy. Solid-state characterization and thermal analysis confirmed that amorphous solid dispersions were formed upon electrospinning. The Insent E-tongue was used to assess the taste-masking efficiency of the samples, and it was found that this formulation was undetectable by the bitter sensor, indicating successful taste-masking compared to the raw version of the drug. The E-tongue also confirmed the drug’s bitterness threshold as compared to quinine HCl dihydrate, a parameter that is useful for formulation design and taste-masking planning.
Highlights
Poor taste of medicines is one of the main adherence challenges for the paediatric population, it is necessary to design specific dosage forms suitable for administration to children [1]
The mean fibre diameter was measured as 565 nm ± 206 nm, which is within the desired nano-range. It can be seen from the image that the fibres were not perfectly bead-free, with some spindle formation. As this is planned to be used as part of a co-axial electrospinning process, there is leeway for the solution to be less electrospinnable than the second solution to be used in the process [16]
These peaks do not seem to present anymore in the fibres which indicates that the functional groups within the drug could have formed hydrogen bonds with the methacrylate polymers. These interactions give an indication of compatibility and stability of the drug in the co-polymer matrix [34]. These results indicate that chlorpheniramine maleate (CPM) was amorphously dispersed in the polymeric carriers, which was validated in the X-ray diffraction (XRD) data
Summary
Poor taste of medicines is one of the main adherence challenges for the paediatric population, it is necessary to design specific dosage forms suitable for administration to children [1]. Age appropriate paediatric medicines have traditionally been in comparatively low abundance, a fact that led to the introduction of the EU 2007 Paediatric Regulation [2]. This legislation stipulates that, for any new drug, the manufacturer is required to develop an accompanying plan on how the medicine can be practically administered to children, formally known as a Paediatric Investigation Plan, or PIP. As part of the Paediatric Regulation, Paediatric Use Marketing Authorizations, or PUMAs, were introduced [3] These incentivized manufacturers to re-formulate existing drugs on the market into age-appropriate formulations through improving various acceptability attributes, most notably taste. This created a significant window of opportunity for formulators to re-design bitter drugs using innovative techniques to produce palatable age appropriate formulations that may be eligible for PUMA status [4]
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