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Pediatric Formulation Optimization Using a Rational Design: Exploring Amorphous Solid Dispersion Technology with

Izabelle Amorim Ferreira Boza1, Stéfani Laise da Silva1, Nicolly Bittencourt Guedes2

  • 1Department of Chemistry, Center for Physical and Mathematical Sciences, Federal University of Santa Catarina, Florianópolis, SC, 88040-900, Brazil.

AAPS Pharmscitech
|January 17, 2025
PubMed

Insights

Developing pediatric antifungal formulations for terbinafine hydrochloride (TER) is challenging due to its low solubility. Researchers identified Soluplus® as a promising carrier for amorphous solid dispersions, enhancing TER solubility and bioavailability in children.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Pediatric Formulations

Background:

  • Pediatric formulations face unique challenges, especially for drugs like terbinafine hydrochloride (TER), an antifungal with low aqueous solubility.
  • Tinea capitis, a common pediatric fungal infection, requires effective oral treatments, but TER's poor solubility hinders oral bioavailability.

Purpose of the Study:

  • To rationally select suitable, pediatric-approved carriers for enhancing TER's apparent solubility.
  • To develop amorphous solid dispersions (ASDs) of TER using spray drying for improved oral bioavailability in pediatric patients.

Main Methods:

  • Evaluated solubility parameters, equilibrium solubility, and pediatric dose numbers for carrier selection.
  • Utilized Plasdone S-360 ULTRA®, HPMCAS L, and Soluplus® as potential carriers.
  • Characterized drug-carrier interactions and solid-state properties using various techniques.
  • Prepared ASDs of TER using spray drying with the selected carrier.

Main Results:

  • Solubility of TER was pH-dependent, with highest solubility observed in pH 6.5 buffer with 10% Soluplus®.
  • Soluplus® yielded the lowest pediatric dose number (0.23) for children over 6 years old.
  • Spray-dried ASDs significantly enhanced TER's apparent solubility and maintained prolonged supersaturation.
  • No phase transitions or significant drug-carrier interactions were observed.

Conclusions:

  • Soluplus® is a suitable carrier for developing TER amorphous solid dispersions for pediatric oral formulations.
  • Spray-dried ASDs of TER with Soluplus® offer a promising strategy to improve oral bioavailability and efficacy in children.
  • This approach addresses the challenges of developing effective oral antifungal treatments for pediatric patients.

Keywords:
amorphous solid dispersionoral drug administrationpediatric formulationrational designsolubilityterbinafine hydrochloride

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