Quercetin topical application, from conventional dosage forms to nanodosage forms

Hatahet, Taher; Morille, Marie; Hommoss, A.; Devoisselle, Jean-Marie; Müller, Rainer H.; Bégu, Sylvie

doi:10.1016/j.ejpb.2016.08.011

Cited by 92 publications

(65 citation statements)

References 96 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…In this study, the primary purpose of formulating QC in ethosomes was to overcome its penetration [27] and bioavailability [39] problems. Ahad et al showed that ethosomes could increase the bioavailability of drugs [39] .…”

Section: Resultsmentioning

confidence: 99%

“…Hydrophilic gels are known to increase drug release quickly [27] . QC has very limited skin penetration capacity.…”

Section: Based Onmentioning

confidence: 99%

“…Also, ethanol can disrupt the lipid bilayer in the stratum corneum [11] . Ethanol provides a higher skin penetration for entrapped molecules compared to conventional liposomes because it facilitates ethosomes penetration [27] . Hatahet et al stated that even QC is formulated in a lipid nanoparticle, it will not show a transdermal delivery on human skin.…”

Section: Based Onmentioning

confidence: 99%

“…Studies related to topical or dermal formulation of QC were done by formulating QC into gel, emulgel and microemulsion gel [27] , microneedles, lipid microparticles [28] and nanocrystals [29] . A previous study on QC ethosomes by Park et al [30] in which QC was formulated into ethosomes to enhance its skin deposition.…”

Section: In Vitro Penetration and Bioavailability Of Novel Transdermamentioning

confidence: 99%

See 3 more Smart Citations

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

Ramadon¹,

Anwar²,

Harahap³

2017

pharmaceutical-sciences

View full text Add to dashboard Cite

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.

show abstract

Section: Resultsmentioning

confidence: 99%

“…Hydrophilic gels are known to increase drug release quickly [27] . QC has very limited skin penetration capacity.…”

Section: Based Onmentioning

confidence: 99%

Section: Based Onmentioning

confidence: 99%

Section: In Vitro Penetration and Bioavailability Of Novel Transdermamentioning

confidence: 99%

See 2 more Smart Citations

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

Ramadon¹,

Anwar²,

Harahap³

2017

pharmaceutical-sciences

View full text Add to dashboard Cite

show abstract

“…However, quercetin application is limited because of its poor water solubility. Recently, quercetin has been formulated in various types such as nanoformulations, deformable liposomes and glycerosomes for overcoming limited water solubility and enhancing its stability [5]. Although these formulations improved its potential compared to their conventional forms with respect to enhanced skin penetration, the optimized solution formula is still lacking [15,16].…”

mentioning

confidence: 99%

Enhancing Antioxidant Cellular Defense by Using Quercetin Loaded TiO2 Nanoparticles in Swiss 3T3 Albino Mouse Fibroblast Cells

Birinci¹,

Niazi²,

Başağa³

2017

J Nanomed Nanotechnol

View full text Add to dashboard Cite

Living organisms are continuously exposed to a wide variety of oxidative radicals. Therefore, there is a constant demand for exogenous antioxidant supply. In this regard, one of these exogenous antioxidants with well established potency, quercetin has been utilized in various formulations. Yet due to its poor water solubility, its extensive applications are limited so far. In this study, TiO 2 nanoparticles (TiO 2 -NPs) were employed to improve the cellular penetration of quercetin and to maximize its antioxidant effects on swiss 3T3 albino mouse fibroblast cells. Surfaces of TiO 2 -NPs were modified with Polyethylene glycol (PEG) that enabled better dispersion and enhanced biocompatibility. Toxicity of quercetin and quercetin loaded TiO 2 NPs (QL-TiO 2 -NPs) were evaluated in terms of cell morphology and measured with cell viability assay. For an in-depth cell viability analysis, key markers of apoptosis were investigated by immunoblotting analysis. As an indicator of apoptotic cell death, cleavage of caspase 3 (Cas 3) and poly (ADP-ribose) polymerase proteins (Parp) were detected in quercetin treated cells. Antioxidant capacity of quercetin in the form of QL-TiO 2 -NPs was measured in the cells in which generation of reactive oxygen species (ROS) and superoxide was induced by pyocyanin. Quantitative ROS measurements were confirmed with confocal microscopy. Further mechanistic insight on upregulation of NF-E2 related factor 2 (NRF2) pathway via QL-TiO 2 -NPs was also provided in an effort to validate its antioxidant defense. Target enzymes of NRF2, heme oxygenase-1 (HO-1), NAD(P)H: quinone oxydoreductase1 (NQO1) and superoxide dismutase1 (SOD1) expressions were increased in the model proposed. QL-TiO 2 -NPs allowed high bioavaliability of quercetin concentration and stability in the cell with maximum antioxidant capacity against formation of ROS without any cytotoxicity. Overall, this paper sheds light on how the efficiency of quercetin in a nanosystem can serve as a safe therapeutic candidate for breaking the vicious ROS cycle in the cell. Citation: Birinci Y, Niazi JH, Basaga H (2017) Enhancing Antioxidant Cellular Defense by Using Quercetin Loaded TiO 2 Nanoparticles in Swiss 3T3Albino Mouse Fibroblast Cells. J Nanomedic Nanotechnol S8: 001. doi:10.4172/2157-7439.S8-001Page 2 of 10 J Nanomedic Nanotechnol Nanotechnology: Challenges and Perspectives in Medicine ISSN: 2157-7439 JNMNT an open access journal 3T3 albino mouse fibroblast cells. Total cellular ROS and superoxide levels in treated cells were determined and compared with those of control cells. However, quercetin in a nanosystem shows maximum antioxidant activity by triggering NRF2 pathway, upregulating phase II antioxidant enzymes, heme oxygenase-1 (HO-1), NAD(P)H: quinone oxydoreductase1 (NQO1) and superoxide dismutase1 (SOD1). In summary, our study demonstrated that quercetin loaded TiO 2 -NPs served as an effective nanosystem for delivering quercetin to swiss 3T3 albino mouse fibroblast cells in vitro and provided protection against oxida...

show abstract

A hydrogel–fiber–hydrogel composite scaffold based on silk fibroin with the dual‐delivery of oxygen and quercetin

Aleemardani

Solouk

Akbari

et al. 2022

Biotech & Bioengineering

View full text Add to dashboard Cite

Supplying sufficient oxygen within the scaffolds is one of the essential hindrances in tissue engineering that can be resolved by oxygen‐generating biomaterials (OGBs). Two main issues related to OGBs are controlling oxygenation and reactive oxygen species (ROS). To address these concerns, we developed a composite scaffold entailing three layers (hydrogel‐electrospun fibers‐hydrogel) with antioxidant and antibacterial properties. The fibers, the middle layer, reinforced the composite structure, enhancing the mechanical strength from 4.27 ± 0.15 to 8.27 ± 0.25 kPa; also, this layer is made of calcium peroxide and silk fibroin (SF) through electrospinning, which enables oxygen delivery. The first and third layers are physical SF hydrogels to control oxygen release, containing quercetin (Q), a nonenzymatic antioxidant. This composite scaffold resulted in almost more than 40 mmHg of oxygen release for at least 13 days, and compared with similar studies is in a high range. Here, Q was used for the first time for an OGB to scavenge the possible ROS. Q delivery not only led to antioxidant activity but also stabilized oxygen release and enhanced cell viability. Based on the given results, this composite scaffold can be introduced as a safe and controllable oxygen supplier, which is promising for tissue engineering applications, particularly for bone.

show abstract

Quercetin topical application, from conventional dosage forms to nanodosage forms

Cited by 92 publications

References 96 publications

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

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

Enhancing Antioxidant Cellular Defense by Using Quercetin Loaded TiO2 Nanoparticles in Swiss 3T3 Albino Mouse Fibroblast Cells

A hydrogel–fiber–hydrogel composite scaffold based on silk fibroin with the dual‐delivery of oxygen and quercetin

Contact Info

Product

Resources

About