Utilising Co-Axial Electrospinning as a Taste-Masking Technology for Paediatric Drug Delivery

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.

Download Full-text

Characterization of Amorphous Solid Dispersions and Identification of Low Levels of Crystallinity by Transmission Electron Microscopy

Molecular Pharmaceutics ◽

10.1021/acs.molpharmaceut.0c00918 ◽

2021 ◽

Author(s):

Mark S’ari ◽

Helen Blade ◽

Stephen Cosgrove ◽

Rik Drummond-Brydson ◽

Nicole Hondow ◽

...

Keyword(s):

Electron Microscopy ◽

Transmission Electron Microscopy ◽

Solid Dispersions ◽

Amorphous Solid ◽

Amorphous Solid Dispersions ◽

Transmission Electron ◽

Low Levels

Download Full-text

ChemInform Abstract: Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

ChemInform ◽

10.1002/chin.201642262 ◽

2016 ◽

Vol 47 (42) ◽

Author(s):

Shrawan Baghel ◽

Helen Cathcart ◽

Niall J. O'Reilly

Keyword(s):

Solid State ◽

Classification System ◽

Solid Dispersions ◽

Amorphous Solid ◽

Class Ii ◽

Amorphous Solid Dispersions ◽

Biopharmaceutical Classification System ◽

Solid State Characterization

Download Full-text

Solid-state characterization of Felodipine–Soluplus amorphous solid dispersions

Drug Development and Industrial Pharmacy ◽

10.3109/03639045.2015.1104347 ◽

2015 ◽

Vol 42 (3) ◽

pp. 485-496 ◽

Cited By ~ 18

Author(s):

Jiannan Lu ◽

Kristina Cuellar ◽

Nathan I. Hammer ◽

Seongbong Jo ◽

Andreas Gryczke ◽

...

Keyword(s):

Solid State ◽

Solid Dispersions ◽

Amorphous Solid ◽

Amorphous Solid Dispersions ◽

Solid State Characterization

Download Full-text

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Journal of Pharmaceutical Sciences ◽

10.1016/j.xphs.2015.10.008 ◽

2016 ◽

Vol 105 (9) ◽

pp. 2527-2544 ◽

Cited By ~ 366

Author(s):

Shrawan Baghel ◽

Helen Cathcart ◽

Niall J. O'Reilly

Keyword(s):

Solid State ◽

Classification System ◽

Solid Dispersions ◽

Amorphous Solid ◽

Class Ii ◽

Amorphous Solid Dispersions ◽

Biopharmaceutical Classification System ◽

Solid State Characterization

Download Full-text

Direct Powder Extrusion 3D Printing of Praziquantel to Overcome Neglected Disease Formulation Challenges in Paediatric Populations

Pharmaceutics ◽

10.3390/pharmaceutics13081114 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1114

Author(s):

Janine Boniatti ◽

Patricija Januskaite ◽

Laís B. da Fonseca ◽

Alessandra L. Viçosa ◽

Fábio C. Amendoeira ◽

...

Keyword(s):

3D Printing ◽

Solid Dispersions ◽

Amorphous Solid ◽

Fold Increase ◽

In Vitro Dissolution ◽

Taste Masking ◽

Fused Deposition Modelling ◽

Amorphous Solid Dispersions ◽

Fused Deposition

For the last 40 years, praziquantel has been the standard treatment for schistosomiasis, a neglected parasitic disease affecting more than 250 million people worldwide. However, there is no suitable paediatric formulation on the market, leading to off-label use and the splitting of commercial tablets for adults. In this study, we use a recently available technology, direct powder extrusion (DPE) three-dimensional printing (3DP), to prepare paediatric Printlets™ (3D printed tablets) of amorphous solid dispersions of praziquantel with Kollidon® VA 64 and surfactants (Span™ 20 or Kolliphor® SLS). Printlets were successfully printed from both pellets and powders obtained from extrudates by hot melt extrusion (HME). In vitro dissolution studies showed a greater than four-fold increase in praziquantel release, due to the formation of amorphous solid dispersions. In vitro palatability data indicated that the printlets were in the range of praziquantel tolerability, highlighting the taste masking capabilities of this technology without the need for additional taste masking excipients. This work has demonstrated the possibility of 3D printing tablets using pellets or powder forms obtained by HME, avoiding the use of filaments in fused deposition modelling 3DP. Moreover, the main formulation hurdles of praziquantel, such as low drug solubility, inadequate taste, and high and variable dose requirements, can be overcome using this technology.

Download Full-text