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Orphan Formulations in Pediatric Schistosomiasis Treatment: Development and Characterization of Praziquantel

M A Gonzalez1,2, M V Ramírez Rigo1,2, N L Gonzalez Vidal3,4

  • 1Departamento de Biología, Bioquímica y Farmacia, Universidad Nacional del Sur (UNS), San Juan 670, 8000, Bahía Blanca, Argentina.

AAPS Pharmscitech
|October 18, 2019
PubMed

Insights

This study developed a praziquantel dry nanosuspension for children, improving bioavailability and compliance. The novel formulation enhances drug dissolution and taste for effective schistosomiasis treatment.

Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Pediatric Pharmacology

Background:

  • Praziquantel is the primary treatment for schistosomiasis but suffers from poor solubility and taste, limiting pediatric use.
  • Low bioavailability and poor patient compliance are significant challenges in pediatric praziquantel administration.
  • Developing palatable and bioavailable praziquantel formulations is crucial for effective pediatric schistosomiasis control.

Purpose of the Study:

  • To develop a dry nanosuspension of praziquantel for pediatric use.
  • To improve praziquantel's bioavailability and patient compliance through taste masking and enhanced dissolution.
  • To create an extemporaneously redispersible powdered formulation suitable for young children.

Main Methods:

  • Combination of high-pressure homogenization and spray drying to create praziquantel nanoparticles.
  • Characterization of formulations including particle size, crystallinity, morphology, and dissolution.
  • Evaluation of sedimentation-redispersibility behavior of the dried nanosuspension.
  • Optimization of stabilizer-to-drug ratios for nanosuspension development.

Main Results:

  • Significant reduction in particle size achieved via high-pressure homogenization.
  • Successful microencapsulation of nanoparticles using spray drying, yielding redispersible powders.
  • Conserved nanometric particle size distribution and crystallinity after drying and redispersion.
  • Enhanced in vitro dissolution performance maintained after the drying and redispersion process.

Conclusions:

  • The developed nanoparticle-loaded powders offer a promising approach for administering praziquantel to preschool-age children.
  • This formulation addresses key challenges of low solubility, poor taste, and bioavailability in pediatric praziquantel therapy.
  • The technology facilitates extemporaneous preparation, improving compliance and therapeutic outcomes for pediatric schistosomiasis.

Keywords:
high-pressure homogenizationorphan formulationspediatricpraziquantelspray drying

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