In Vivo and In Vitro Taste Assessment of Artesunate-Mefloquine, Praziquantel, and Benznidazole Drugs for Neglected Tropical Diseases and Pediatric Patients

AAPS PharmSciTech. 2021 Dec 14;23(1):22. doi: 10.1208/s12249-021-02162-z.

Abstract

The assessment of drug taste is crucial for pediatric treatments so that formulations can be developed to enhance their effectiveness. In this study, in vivo and in vitro methods were applied to evaluate the taste of tablets of three drugs administered to children without taste-masking excipients to treat tropical diseases, namely artesunate-mefloquine (ASMQ), praziquantel (PZQ), and benznidazole (BNZ). In the first method, a model of rat palatability was adapted with recirculation to ensure sample dispersion, and the data were analyzed using ANOVA (single factor, 95%). The taste assessment results (in vivo) indicated an aversion to the three medicines, denoted by the animals retracting themselves to the bottom of the box after the first contact with the drugs. For the placebo samples, the animals behaved normally, indicating that taste perception was acceptable. The second method was based on the in vitro analysis of capacitance data from a homemade impedimetric electronic tongue. Consistent with the in vivo taste assessment results, the data points obtained with PZQ, ASMQ, and BNZ were far away from those of their placebos in a map built with the multidimensional projection technique referred to as Interactive Document Mapping (IDMAP). A combined analysis of the results with the two methods allowed us to confirm the bitterness of the three drugs, also pointing to electronic tongues as a promising tool to replace in vivo palatability tests.

Keywords: Artesunate-mefloquine; Benznidazole; Electronic tongue; Modified taste aversion model; Off-label use; Pediatric treatment; Praziquantel.

MeSH terms

  • Animals
  • Artesunate
  • Child
  • Humans
  • Mefloquine*
  • Nitroimidazoles
  • Praziquantel*
  • Rats
  • Tablets
  • Taste

Substances

  • Nitroimidazoles
  • Tablets
  • Artesunate
  • Praziquantel
  • Mefloquine
  • benzonidazole