In vitro Penetration and Bioavailability of Novel Transdermal Quercetin-loaded Ethosomal Gel

Abstract

Quercetin has been widely used to treat many diseases because of its high antioxidant activity. However, it has low oral bioavailability and penetration through the skin. The aim of this research was to enhance penetration and bioavailability of quercetin using transdermal ethosomal gel. Three ethosomal formulae, E1 (1 %), E2 (1.5 %) and E3 (2 %) with different concentration of quercetin were prepared using thin-film hydration method. Their physical properties were characterized, and then a selected ethosomal formula was incorporated into a gel dosage form. Two gels, one ethosomal and the other non-ethosomal were prepared. In vitro penetration using Franz diffusion cells and bioavailability study in Sprague Dawley male rats were carried out. Results showed that E2 was the chosen formula to be incorporated into the gel dosage form. According to the in vitro penetration study, the diffusion flux of quercetin from the ethosomal and non-ethosomal gels were 343.35±17.69 ng/cm 2 /h and 120.68±11.92 ng/cm 2 /h, respectively (P<0.05). In the bioavailability study, ethosomal gel showed higher maximum concentration (C max ) and area under curve (AUC 0-t ) when compared to non-ethosomal gel and oral suspension. C max from the ethosomal gel, nonethosomal gel, and oral suspension were 413.49±28.64, 189.46±49.68, and 61.92±14.31 ng/ml, respectively (P<0.05). AUC 0-t from the ethosomal gel, non-ethosomal gel, and oral suspension were 4035.15±560.60, 584.87±265.46, and 431.21±239.85, respectively (P<0.05). In conclusion, ethosomal gel could increase penetration and bioavailability of quercetin compared to non-ethosomal gel.

Antioxidant Activities of Quercetin and Its Complexes for Medicinal Application

“…When it forms complexes with metal ions or complex ions, its bioavailability and antioxidant effect are enhanced and strengthened. In addition to quercetin complexes, newer preparations of quercetin have emerged in recent years, including nanoparticles loaded with quercetin [105,106,107], polymeric micelles of quercetin [108], quercetin-loaded mucoadhesive nanoemulsion [109], quercetin-loaded gel [110], and others [111,112]. These preparations improve the solubility and bioavailability of quercetin, which enhances its clinical efficacy and offers new drug formulations for research and development.…”

Formulation of Transfersomal Green Tea (Camellia sinensis L. Kuntze) Leaves Extract Cream and In Vitro Penetration Study Using Franz Difussion Cell

“…25 It is because they would have tend to repel each other, and they would not aggregate to become a larger particle. 26 The value of zeta potential for all formulations were less than -30 mV. It indicated that all formulations might have a good stability.…”

Anti-inflammatory Activity of Nanoemulgel formulated from Ageratum conyzoides (L.) L. and Oldenlandia corymbosa L. Extracts in Rats

“…The challenge of a study that uses dosage form for transdermal delivery is to improve the penetration through the skin to act locally or systemically. For transdermal delivery, nanoemulsion 18 , nanoparticle 10 , ethosome 20 , nanostructured lipid carriers (NLC) 21 , solid lipid nanoparticle (SLN) 22 loaded quercetin (an active compound of ACE-OCE) have been developed to improve skin penetration.…”