Pharmaceutics (Jun 2023)

Biocomposite for Prolonged Release of Water-Soluble Drugs

  • Lyghia M. A. Meirelles,
  • Raquel de Melo Barbosa,
  • Renato Ferreira de Almeida Júnior,
  • Paula Renata Lima Machado,
  • Luana Perioli,
  • César Viseras,
  • Fernanda Nervo Raffin

DOI
https://doi.org/10.3390/pharmaceutics15061722
Journal volume & issue
Vol. 15, no. 6
p. 1722

Abstract

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This study aimed to develop a prolonged-release system based on palygorskite and chitosan, which are natural ingredients widely available, affordable, and accessible. The chosen model drug was ethambutol (ETB), a tuberculostatic drug with high aqueous solubility and hygroscopicity, which is incompatible with other drugs used in tuberculosis therapy. The composites loaded with ETB were obtained using different proportions of palygorskite and chitosan through the spray drying technique. The main physicochemical properties of the microparticles were determined using XRD, FTIR, thermal analysis, and SEM. Additionally, the release profile and biocompatibility of the microparticles were evaluated. As a result, the chitosan–palygorskite composites loaded with the model drug appeared as spherical microparticles. The drug underwent amorphization within the microparticles, with an encapsulation efficiency greater than 84%. Furthermore, the microparticles exhibited prolonged release, particularly after the addition of palygorskite. They demonstrated biocompatibility in an in vitro model, and their release profile was influenced by the proportion of inputs in the formulation. Therefore, incorporating ETB into this system offers improved stability for the administered product in the initial tuberculosis pharmacotherapy dose, minimizing its contact with other tuberculostatic agents in the treatment, as well as reducing its hygroscopicity.

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