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<p>Flavonoids present in <i>Passiflora</i> species are phenolic compounds with large neuropharmacological activity, but their physicochemical properties limit their pharmaceutical applications. In this sense, self-assembled polymeric nanoparticles were prepared by nanoencapsulation of a flavonoid-rich fraction from the leaves of <i>Passiflora edulis f. flavicarpa</i> O. Deg., Passifloraceae, into Eudragit E PO polymethylmethacrylate copolymer by using the solvent displacement method. The flavonoid-rich fraction from <i>P. edulis</i> leaf extract was obtained by eco-friendly fractionation techniques, and it exhibited high total flavonoid content (37.1%; 371.38&#xa0;mg/g), and fifteen <i>C</i> and/or <i>O</i>-glycosyl flavones molecules were putatively identified by LC–MS/MS. The addition of the flavonoid-rich fraction at different weight percent loadings of nanoparticles was investigated. The morphology, physical–chemical properties, and stability of nanoparticles were characterized through size and zeta potential measurements, infrared spectroscopy, atomic absorption microscopy, and efficiency entrapment by UHPLC-UV-DAD. Assessment of <i>in vivo</i> biocompatibility and antidepressant-like activity and effects on spontaneous locomotion were investigated in mice. The developed flavonoid-rich fraction nanoparticles exhibited good smallsize and spherical shape, high content, and encapsulation efficiency of bioactive flavonoids, good biocompatibility, and increased antidepressant efficacy (tenfold) compared to the free flavonoid-rich fraction. The small size and positive charge make these nanoparticles containing the flavonoid-rich fraction a potential active pharmaceutical ingredient for targeting neuroactive flavonoids to the central nervous system.</p> Graphical Abstract <p></p>

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Nanotechnology Combined with Eco-Friendly Refinement as an Innovative Drug Delivery Approach for Passiflora edulis f. flavicarpa—An Antidepressant Flavonoid-Rich Fraction–Loaded Biocompatible Nanoparticle

  • 期刊论文

  • 发表日期：

    2025年8月7日

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  • Jovelina Samara Ferreira Alves,
  • Alaine Maria dos Santos Silva,
  • José Ivan Marques de Medeiros,
  • Lucas Silva Abreu,
  • Layse Raynara Ferreira Costa,
  • Thaís Gomes de Carvalho,
  • Edilane Rodrigues Dantas de Araújo,
  • Marcela Abbott Galvão Ururahy,
  • Raimundo Fernandes de Araújo-Júnior,
  • Josean Fechine Tavares,
  • Norberto Peporine Lopes,
  • Leandro De Santis Ferreira,
  • Elaine Cristina Gavioli,
  • Arnóbio Antônio da Silva-Júnior,
  • Silvana Maria Zucolotto

摘要

Flavonoids present in Passiflora species are phenolic compounds with large neuropharmacological activity, but their physicochemical properties limit their pharmaceutical applications. In this sense, self-assembled polymeric nanoparticles were prepared by nanoencapsulation of a flavonoid-rich fraction from the leaves of Passiflora edulis f. flavicarpa O. Deg., Passifloraceae, into Eudragit E PO polymethylmethacrylate copolymer by using the solvent displacement method. The flavonoid-rich fraction from P. edulis leaf extract was obtained by eco-friendly fractionation techniques, and it exhibited high total flavonoid content (37.1%; 371.38 mg/g), and fifteen C and/or O-glycosyl flavones molecules were putatively identified by LC–MS/MS. The addition of the flavonoid-rich fraction at different weight percent loadings of nanoparticles was investigated. The morphology, physical–chemical properties, and stability of nanoparticles were characterized through size and zeta potential measurements, infrared spectroscopy, atomic absorption microscopy, and efficiency entrapment by UHPLC-UV-DAD. Assessment of in vivo biocompatibility and antidepressant-like activity and effects on spontaneous locomotion were investigated in mice. The developed flavonoid-rich fraction nanoparticles exhibited good smallsize and spherical shape, high content, and encapsulation efficiency of bioactive flavonoids, good biocompatibility, and increased antidepressant efficacy (tenfold) compared to the free flavonoid-rich fraction. The small size and positive charge make these nanoparticles containing the flavonoid-rich fraction a potential active pharmaceutical ingredient for targeting neuroactive flavonoids to the central nervous system.

Graphical Abstract