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Hybrid Nanobeads for Oral Indomethacin Delivery.

Flávia Monique Rocha BonettiEneida de PaulaBelchiolina Beatriz FonsecaGabriela Ribeiro da SilvaLeandro Santana Soares da SilvaLudmilla David de MouraMárcia Cristina BreitkreitzGustavo H Rodrigues da SilvaLigia Nunes de Morais Ribeiro
Published in: Pharmaceutics (2022)
The oral administration of the anti-inflammatory indomethacin (INDO) causes severe gastrointestinal side effects, which are intensified in chronic inflammatory conditions when a continuous treatment is mandatory. The development of hybrid delivery systems associates the benefits of different (nano) carriers in a single system, designed to improve the efficacy and/or minimize the toxicity of drugs. This work describes the preparation of hybrid nanobeads composed of nanostructured lipid carriers (NLC) loading INDO (2%; w / v ) and chitosan, coated by xanthan. NLC formulations were monitored in a long-term stability study (25 °C). After one year, they showed suitable physicochemical properties (size < 250 nm, polydispersity < 0.2, zeta potential of -30 mV and spherical morphology) and an INDO encapsulation efficiency of 99%. The hybrid (lipid-biopolymers) nanobeads exhibited excellent compatibility between the biomaterials, as revealed by structural and thermodynamic properties, monodisperse size distribution, desirable in vitro water uptake and prolonged in vitro INDO release (26 h). The in vivo safety of hybrid nanobeads was confirmed by the chicken embryo (CE) toxicity test, considering the embryos viability, weights of CE and annexes and changes in the biochemical markers. The results point out a safe gastro-resistant pharmaceutical form for further efficacy assays.
Keyphrases
  • oxidative stress
  • anti inflammatory
  • fatty acid
  • risk assessment
  • pregnant women
  • high throughput
  • high resolution
  • replacement therapy
  • combination therapy
  • energy transfer
  • oxide nanoparticles
  • simultaneous determination