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<p>A spray-dried hydroethanolic leaf extract of <i>Celtis iguanaea</i> (Jacq.) Sarg., Cannabaceae, was developed and evaluated for its gastroprotective efficacy in mice. A 3<sup>3</sup> Box-Behnken design (n = 15) and Response Surface Methodology were used to optimize the spray drying. The variables studied were drying air inlet temperature (100 – 140&#xa0;°C), extract feed flow rate (0.3 – 0.7&#xa0;l/h), and leucine content (15 – 45% m/m relative to solids) as a drying aid. The inlet temperature and leucine content were the main factors affecting the drying process. Optimal conditions were an air inlet of 120&#xa0;°C, an extract feed flow rate of 0.3&#xa0;l/h, and a leucine content of 45%, achieving a yield of 52% with microparticles of 3.4&#xa0;µm. However, energy efficiency requires improvements. The optimized spray-dried hydroethanolic leaf extract of <i>C. iguanaea</i> contained 21.8&#xa0;mg/g total polyphenols, 49.7&#xa0;mg/g flavonoids, and 518.8&#xa0;mg/g phytosterols, with an IC<sub>50</sub> of 301.6&#xa0;µg/ml and an electrochemical index of 6.1 µA/V. LC-UV, ESI(-)-MS, and LC-PDA analyses identified hydroxycinnamic acid and two flavones as major compounds. Regardless of the use of leucine as a drying aid, spray drying proved more effective than freeze drying in preserving bioactive compounds. In an indomethacin-induced gastric ulcer model, spray-dried hydroethanolic leaf extract of <i>C. iguanaea</i> (150 and 300&#xa0;mg/kg, <i>p.o</i>.) significantly reduced the lesion index, potentially due to its immunomodulatory effects, including decreased IL-1β and increased IL-10 levels in the stomach. This Quality by Design approach successfully developed a high-value phytopharmaceutical intermediate product with favorable yield, antioxidant properties, and <i>in vivo</i> gastroprotective efficacy. Further studies on stability, pharmacokinetics, drug interactions, and human safety are needed to support its use in Brazilian complementary medicine<i>.</i></p> Graphical Abstract <p></p>

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Quality-by-design Development of Celtis iguanaea Microparticles with In vivo Gastroprotective Efficacy

  • 期刊论文

  • 发表日期：

    2025年8月11日

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  • Rúbia Bellard e Silva,
  • José Luís Rodrigues Martins,
  • Dionys de Souza Almeida,
  • Gabriela Viana Ferreira,
  • Kátia Regina Ribeiro,
  • Mairon César Coimbra,
  • Laura Jéssica Pereira,
  • Emmilly de Oliveira Alves,
  • Marx Osório Araújo Pereira,
  • Eric de Souza Gil,
  • Rodolfo de Paula Vieira,
  • André Luís Lacerda Bachi,
  • Jônatas Bussador do Amaral,
  • Gustavo Fernando de Frazão Lima,
  • José Augusto Ferreira Perez Villar,
  • Camile Aparecida da Silva,
  • James Oluwagbamigbe Fajemiroye,
  • Elson Alves Costa,
  • Renê Oliveira do Couto

摘要

A spray-dried hydroethanolic leaf extract of Celtis iguanaea (Jacq.) Sarg., Cannabaceae, was developed and evaluated for its gastroprotective efficacy in mice. A 33 Box-Behnken design (n = 15) and Response Surface Methodology were used to optimize the spray drying. The variables studied were drying air inlet temperature (100 – 140 °C), extract feed flow rate (0.3 – 0.7 l/h), and leucine content (15 – 45% m/m relative to solids) as a drying aid. The inlet temperature and leucine content were the main factors affecting the drying process. Optimal conditions were an air inlet of 120 °C, an extract feed flow rate of 0.3 l/h, and a leucine content of 45%, achieving a yield of 52% with microparticles of 3.4 µm. However, energy efficiency requires improvements. The optimized spray-dried hydroethanolic leaf extract of C. iguanaea contained 21.8 mg/g total polyphenols, 49.7 mg/g flavonoids, and 518.8 mg/g phytosterols, with an IC50 of 301.6 µg/ml and an electrochemical index of 6.1 µA/V. LC-UV, ESI(-)-MS, and LC-PDA analyses identified hydroxycinnamic acid and two flavones as major compounds. Regardless of the use of leucine as a drying aid, spray drying proved more effective than freeze drying in preserving bioactive compounds. In an indomethacin-induced gastric ulcer model, spray-dried hydroethanolic leaf extract of C. iguanaea (150 and 300 mg/kg, p.o.) significantly reduced the lesion index, potentially due to its immunomodulatory effects, including decreased IL-1β and increased IL-10 levels in the stomach. This Quality by Design approach successfully developed a high-value phytopharmaceutical intermediate product with favorable yield, antioxidant properties, and in vivo gastroprotective efficacy. Further studies on stability, pharmacokinetics, drug interactions, and human safety are needed to support its use in Brazilian complementary medicine.

Graphical Abstract