Quercetin in w/o microemulsion: In vitro and in vivo skin penetration and efficacy against UVB-induced skin damages evaluated in vivo

Vicentini, Fabiana T. M. C.; Simi, Thais R. M.; Ciampo, José Orestes Del; Wolga, Nilce O.; Pitol, Dimítrius Leonardo; Iyomasa, Mamie Mizusaki; Bentley, Maria Vitória Lopes Badra; Fonseca, Maria José Vieira

doi:10.1016/j.ejpb.2008.01.012

Cited by 173 publications

(119 citation statements)

References 36 publications

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“…Although topically applied surfactants have the potential to solubilize lipids in the stratum corneum and lead to an increased flow of substances through the skin (46), literature data show that non-ionic surfactants such as polysorbate have less enhancer effect in human skin while ionic surfactants show more pronounced effects (47). Furthermore, the literature has also reported the use of polysorbate 20 as an adjuvant to acceptor media for in vitro experiments (48,49).…”

Section: Discussionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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Abstract. Transdermal delivery of non-steroidal anti-inflammatory drugs may be an interesting strategy for delivering these drugs to the diseased site, but it would be ineffective due to low skin permeability. We investigated whether oleic acid (OA), a lipid penetration enhancer in poloxamer gels named poloxamer-based delivery systems (PBDS), can improve lumiracoxib (LM) delivery to/through the skin. The LM partition coefficient (K) studies were carried out in order to evaluate the drug lipophilicity grade (K octanol/buffer ), showing values >1 which demonstrated its high lipophilicity. Both in vitro percutaneous absorption and skin retention studies of LM were measured in the presence or absence of OA (in different concentrations) in PBDS using porcine ear skin. The flux of in vitro percutaneous absorption and in vitro retention of LM in viable epidermis increased in the presence of 10.0% (w/w) OA in 25.0% (w/w) poloxamer gel. In vivo cutaneous irritation potential was carried out in rabbits showing that this formulation did not provide primary or cumulative cutaneous irritability in animal model. The results showed that 25.0% poloxamer gel containing 10.0% OA is potential transdermal delivery system for LM.KEY WORDS: in vitro skin permeation; lumiracoxib; oleic acid; poloxamer-based delivery systems; skin delivery.

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Section: Discussionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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“…Some silybin was found in skin extracts; however, the detected quantities from all formulations were insignificant but all formulations were significantly different when compared to the ethanolic solution. As shown by Vicentini et al [25], the topical quercetin W/O microemulsion successfully prevented the UVB-induced skin damages using hairless mice with no transdermal delivery. Additionally, several previous studies showed the benefits of silybin to the keratinocytes [26] and melanocytes [27] in which both cells locate in the skin's epidermis.…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 87%

Formulation of Microemulsion Systems for Dermal Delivery of Silymarin

2012

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Abstract. Silymarin is a standardized extract from Silybum marianum seeds, known for its many skin benefits such as antioxidant, anti-inflammatory, and immunomodulatory properties. In this study, the potential of several microemulsion formulations for dermal delivery of silymarin was evaluated. The pseudo-ternary phase diagrams were constructed for the various microemulsion formulations which were prepared using glyceryl monooleate, oleic acid, ethyl oleate, or isopropyl myristate as the oily phase; a mixture of Tween 20®, Labrasol®, or Span 20® with HCO-40® (1:1 ratio) as surfactants; and Transcutol® as a cosurfactant. Oil-inwater microemulsions were selected to incorporate 2% w/w silymarin. After six heating-cooling cycles, physical appearances of all microemulsions were unchanged and no drug precipitation occurred. Chemical stability studies showed that microemulsion containing Labrasol® and isopropyl myristate stored at 40°C for 6 months showed the highest silybin remaining among others. The silybin remainings depended on the type of surfactant and were sequenced in the order of: Labrasol®>Tween 20®>Span 20®. In vitro release studies showed prolonged release for microemulsions when compared to silymarin solution. All release profiles showed the best fits with Higuchi kinetics. Non-occlusive in vitro skin permeation studies showed absence of transdermal delivery of silybin. The percentages of silybin in skin extracts were not significantly different among the different formulations (p>0.05). Nevertheless, some silybin was detected in the receiver fluid when performing occlusive experiments. Microemulsions containing Labrasol® also were found to enhance silymarin solubility. Other drug delivery systems with occlusive effect could be further developed for dermal delivery of silymarin.

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“…Numerous in vitro studies have revealed diverse biological effects of quercetin including antioxidant activity, which can be explained by its metal ion chelations, inhibition of lipid peroxidation and scavenging of oxygen radicals (7,8). Recently, it was demonstrated that topical formulations containing quercetin inhibit UVB-induced cutaneous oxidative stress and inflammation (9,10).…”

Section: Introductionmentioning

confidence: 99%

Quercetin in Lyotropic Liquid Crystalline Formulations: Physical, Chemical and Functional Stability

et al. 2008

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Abstract. The purpose of this study was to develop a lyotropic liquid crystalline formulation using the emulsifier vitamin E TPGS and evaluate its behavior after incorporation of a flavonoid, quercetin. The physical (macro and microscopic), chemical (determination of quercetin content by the HPLC method) and functional (determination of quercetin antioxidant activity by DPPH• assay) stability of the lamellar liquid crystalline formulation containing flavonoid was evaluated when stored at 4±2°C; 30±2°C/70± 5% RH (relative humidity) and 40±2°C/70±5% RH during 12 months. The lamellar liquid crystalline structure of the formulation was maintained during the experiment, however chemical and functional stability results showed a great influence of the storage period in all conditions tested. A significant decrease in quercetin content (approximately 40%) was detected during the first month of storage and a similar significant loss in antioxidant activity was detected after 6 months. The remaining flavonoid content was unchanged during the final 6 months of the experimental period. The results suggest possible interactions between quercetin and the liquid crystalline formulation, which could inhibit or reduce the quercetin activity incorporated in the system. In conclusion, the present study demonstrated that incorporation of quercetin (1%) did not affect the liquid crystalline structure composed of vitamin E TPGS/IPM/PG-H 2 O (1:1) at 63.75/21.25/15 (w/w/w). Nevertheless, of the total quercetin incorporated in the system only 60% was free to act as an antioxidant.

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Quercetin in w/o microemulsion: In vitro and in vivo skin penetration and efficacy against UVB-induced skin damages evaluated in vivo

Cited by 173 publications

References 36 publications

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

Formulation of Microemulsion Systems for Dermal Delivery of Silymarin

Quercetin in Lyotropic Liquid Crystalline Formulations: Physical, Chemical and Functional Stability

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