<p>Chrysin, a flavonoid effective against various skin cancers, displays poor solubility, skin permeation, and bioavailability. Emulgel emerges as an innovative and promising strategy for the topical administration of chrysin, offering significant advantages over existing systems. Passion fruit oil (PFO) enhances topical formulations with improved safety, compatibility, and drug delivery. However, current emulgels raise safety concerns due to their surfactant, co-surfactant, and oily co-solvent content. This study aimed to develop innovative emulgel containing PFO, without unsafe surfactants, for the topical delivery of chrysin. ATR-FTIR and DSC analyses of chrysin and excipients were performed. A 3<sup>3</sup>-factorial design was used, and the formulations were evaluated for preliminary physicochemical stability, mechanical and rheological properties, i<i>n-vitro</i> release profile of chrysin, bioadhesion and <i>ex-vivo</i> skin permeation by photoacoustic spectroscopy (PAS). ATR-FTIR and DSC analyses confirmed the compatibility of chrysin with the formulation excipients. Formulations F6, F11, and F21 were stable and exhibited hardness (0.2006—0.4299 N), compressibility (1.4737—3.4300 N.mm), elasticity (0.9924 – 1.0034&#xa0;mm), adhesiveness (0.8077—2.2217 N.mm), cohesiveness (0.7637 – 0.8733), softness index (0.0648 – 0.1525 N), and bioadhesive strength (0.0648 – 0.0754 N), both values with relative standard deviation less than 9%. They were pseudoplastic with yield value, thixotropy, and viscoelasticity. Chrysin release profile was slow and governed by anomalous transport. PAS analysis showed chrysin could permeate the stratum corneum and epidermis, reaching the dermal layer. The selected emulgels are promising for effective topical application, and the formulation F21 standing out in particular for further both <i>in vitro</i> and <i>in vivo</i> biological evaluations.</p> Graphical Abstract <p></p>

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Design of Passion Fruit Oil Emulgel for Topical Chrysin Delivery and Ex Vivo Evaluation of Skin Permeation by Photoacoustic Spectroscopy

  • Bruna Gheller de Souza,
  • Lidiane Vizioli de Castro Hoshino,
  • Thalita Schilive Faccin,
  • Mauro Luciano Baesso,
  • Fernanda Belincanta Borghi-Pangoni,
  • Marcos Luciano Bruschi

摘要

Chrysin, a flavonoid effective against various skin cancers, displays poor solubility, skin permeation, and bioavailability. Emulgel emerges as an innovative and promising strategy for the topical administration of chrysin, offering significant advantages over existing systems. Passion fruit oil (PFO) enhances topical formulations with improved safety, compatibility, and drug delivery. However, current emulgels raise safety concerns due to their surfactant, co-surfactant, and oily co-solvent content. This study aimed to develop innovative emulgel containing PFO, without unsafe surfactants, for the topical delivery of chrysin. ATR-FTIR and DSC analyses of chrysin and excipients were performed. A 33-factorial design was used, and the formulations were evaluated for preliminary physicochemical stability, mechanical and rheological properties, in-vitro release profile of chrysin, bioadhesion and ex-vivo skin permeation by photoacoustic spectroscopy (PAS). ATR-FTIR and DSC analyses confirmed the compatibility of chrysin with the formulation excipients. Formulations F6, F11, and F21 were stable and exhibited hardness (0.2006—0.4299 N), compressibility (1.4737—3.4300 N.mm), elasticity (0.9924 – 1.0034 mm), adhesiveness (0.8077—2.2217 N.mm), cohesiveness (0.7637 – 0.8733), softness index (0.0648 – 0.1525 N), and bioadhesive strength (0.0648 – 0.0754 N), both values with relative standard deviation less than 9%. They were pseudoplastic with yield value, thixotropy, and viscoelasticity. Chrysin release profile was slow and governed by anomalous transport. PAS analysis showed chrysin could permeate the stratum corneum and epidermis, reaching the dermal layer. The selected emulgels are promising for effective topical application, and the formulation F21 standing out in particular for further both in vitro and in vivo biological evaluations.

Graphical Abstract