Enhanced transdermal deposition and characterization of quercetin-loaded ethosomes

Park, Soo Nam; Lee, Hye Jin; Kim, Hae Soo; Park, Min A.; Gu, Hyun A

doi:10.1007/s11814-012-0171-4

Cited by 22 publications

(16 citation statements)

References 19 publications

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“…The highest % EE was E2, which was twice higher than E3. This result was similar to Park et al [30] , where the increasing amount of QC incorporated into ethosomes would increase the % EE. This phenomenon was related to the ratio of QC and Phospholipon 80H.…”

Section: Resultssupporting

confidence: 91%

“…It is restricted by both insolubilities in water and the hydrophobic partition coefficient (log P=1.82±0.32) due to the nonpolar groups in its structure [53] . Based on the results of Park et al [30] , cumulative amount of QC penetrated from ethanolic solution and distilled water were only 1.4±0.4 and 0.6±0.2 µg/cm 2 , respectively. These results showed that the cumulative amount QC penetrated would be so small if there were not any treatments or modifications.…”

Section: Based Onmentioning

confidence: 94%

“…A previous study on QC ethosomes by Park et al [30] in which QC was formulated into ethosomes to enhance its skin deposition. However, they only obtained permeation and skin deposition data.…”

Section: In Vitro Penetration and Bioavailability Of Novel Transdermamentioning

confidence: 99%

“…QC ethosomes was prepared by using thin-film hydration method according to Park et al [30] . Three ethosomal formulae were presented in Table 1.…”

Section: Preparation Of Qc Ethosomesmentioning

confidence: 99%

“…The primary content of ethosomes is phospholipid and ethanol. Ethanol increases the elasticity and flexibility of ethosomes so that it can penetrate through the stratum corneum freely [14,15,30] . Also, ethanol can disrupt the lipid bilayer in the stratum corneum [11] .…”

Section: Based Onmentioning

confidence: 99%

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

Ramadon¹,

Anwar²,

Harahap³

2017

pharmaceutical-sciences

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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.

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Section: Resultssupporting

confidence: 91%

Section: Based Onmentioning

confidence: 94%

Section: In Vitro Penetration and Bioavailability Of Novel Transdermamentioning

confidence: 99%

“…QC ethosomes was prepared by using thin-film hydration method according to Park et al [30] . Three ethosomal formulae were presented in Table 1.…”

Section: Preparation Of Qc Ethosomesmentioning

confidence: 99%

Section: Based Onmentioning

confidence: 99%

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

Ramadon¹,

Anwar²,

Harahap³

2017

pharmaceutical-sciences

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Preparation, Physical Characterization, and In Vitro Skin Permeation of Deformable Liposomes Loaded with Taxifolin and Taxifolin Tetraoctanoate

Kim

Jang

et al. 2019

Euro J Lipid Sci & Tech

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This research focuses on deformable liposomes that have great potential as carriers of transdermal drug delivery. In this study, deformable liposomes are prepared using the natural surfactants polyglyceryl‐2 caprate and polyglyceryl‐10 stearate along with phosphatidylcholine and cholesterol to enhance skin penetration of taxifolin and taxifolin tetraoctanoate. Sizes of liposomes made with polyglyceryl‐2 caprate and polyglyceryl‐10 stearate are 64.70–91.30 and 90.20–110.70 nm, respectively. Then entrapment efficiencies and deformability indices are measured, respectively. Liposomes containing 30% surfactant have been selected because they have high entrapment efficiency, stability, and deformability. Crystallization and skin permeation are then measured. Crystallinity is compared using differential scanning calorimetry (DSC). Deformable liposomes containing 30% PGL‐2 caprate and carrying taxifolin tetraoctanoate (CDLTO3) have the lowest melting point (7.55 °C), equivalenting to its highest deformability index. The liposomes are observed by transmission electron microscopy (TEM). Skin permeation studies using Franz cells show that deformable liposomes increased drug permeation more than 1,3‐butylene glycol (1,3‐BG) and control liposomes without surfactant. In particular, when CDLTO3 is used, the amounts of taxifolin tetraoctanoate present in the stratum corneum and skin as well as the amount of permeation are greatest. In conclusion, deformable liposomes containing polyglyceryl‐2 caprate can be effective carriers for taxifolin, taxifolin tetraoctanoate. Practical Applications: Taxifolin is a flavonoid with antioxidative, antibacterial, anti‐inflammatory, and skin‐whitening properties. It would be useful in skin treatments and cosmetics if not for its poor stability. This study develops and characterizes a deformable liposome delivery method that can carry a taxifolin derivative with increased stability and provide better skin penetration compared to conventional liposome. The results can be applied to more effectively deliver beneficial drugs into the skin. Deformable liposomes using the natural surfactants polyglyceryl‐2 caprate and polyglyceryl‐10 stearate increase drug permeation more than did general liposomes. Taxifolin‐tetraoctanoate‐loaded deformable liposomes have the greatest skin permeation.

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Enhanced skin delivery and characterization of rutin-loaded ethosomes

Park

Lee

2014

Korean J. Chem. Eng.

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Enhanced transdermal deposition and characterization of quercetin-loaded ethosomes

Cited by 22 publications

References 19 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

Preparation, Physical Characterization, and In Vitro Skin Permeation of Deformable Liposomes Loaded with Taxifolin and Taxifolin Tetraoctanoate

Enhanced skin delivery and characterization of rutin-loaded ethosomes

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