Zingiber officinale Roscoe(ginger)is traditionally used as a culinary spice worldwide.In folklore medicine,raw and fresh ginger has been used for treating nausea and vomiting,to improve liver function and digestion,an...Zingiber officinale Roscoe(ginger)is traditionally used as a culinary spice worldwide.In folklore medicine,raw and fresh ginger has been used for treating nausea and vomiting,to improve liver function and digestion,antidiarrheal,to treat menstrual cramps,and as an aphrodisiac.Zingerone[4-(4-hydroxy-3-methoxyphenyl)-2-butanone]is the major bioactive ingredient present in ginger.Zingerone has shown a wide-range of pharmacological activities in vitro and in vivo studies.While zingerone is present in small amount in fresh ginger,but its level is increased during drying or heating during cooking.The amount of zingerone increases significantly due to the conversion of gingerol into zingerone through retro-aldol reaction.Owing to its strong antioxidant and anti-inflammatory properties,zingerone has the ability to scavenge reactive oxygen species and to assist in curing a wide array of non-communicable diseases associated with oxidative stress such as diabetes mellitus,obesity,cardiometabolic and cardiovascular disorders,neurological abnormalities,osteoarthritic,and certain cancer types.For this review,extensive literature searches were performed using PubMed,Google Scholar,Science Direct,and other search engines.The major aims of our review are to describe the chemical characteristics of zingerone as well as the various in vitro and in vivo studies reported regarding the pharmacological effects of zingerone and the mechanism of action observed at the cellular and molecular levels.The results of published preclinical and few clinical studies suggest that zingerone has several promising therapeutic applications due to its strong antioxidant,antiinflammatory and anti-proliferative activities without any serious side effects.However,well-designed,randomized,placebo-controlled,and multi-center clinical studies are needed to determine the optimal therapeutic doses,and longterm safety of zingerone.展开更多
Transdermal drug delivery offers the benefits of first-pass metabolism avoidance,high bioavailability,a low dose,and high patient compliance.Ethosomes are lipid-based vesicles containing phospholipids,ethanol,and wate...Transdermal drug delivery offers the benefits of first-pass metabolism avoidance,high bioavailability,a low dose,and high patient compliance.Ethosomes are lipid-based vesicles containing phospholipids,ethanol,and water that enhance drug penetration by overcoming the barrier of the skin.Ethosomes can encapsulate lipophilic as well as hydrophilic drugs to increase their efficacy.Zingerone(ZNE)is a major component found in gingerroot and has potent antidiabetic,antioxidant,and antispasmodic activities.ZNE has low solubility in aqueous media,which leads to low oral bioavailability.ZNE-loaded ethosomes were prepared via the cold method.The ethosomes were optimized by a 3-level and 2-factor full factorial design.The independent variables selected were ethanol(%)and soy lecithin(%).The dependent variables selected were flux(μg/cm^(2)/h)and entrapment efficiency(%).The optimized formulation was evaluated for size,polydispersity index,zeta potential,entrapment efficiency,in vitro drug release,and ex vivo skin drug permeation.The optimized formulation had an average vesicle size of 77.12±1.89 nm,a polydispersity index of 0.350±0.013,a zeta potential of -56.9±1.25 mV,an entrapment efficiency of 75.83%±1.53%,in vitro drug release of 85.97%±1.92%(after 24 h),and ex vivo skin drug permeation of 78.52%±1.62%.The optimized formulation was converted to a gel formulation and characterized for in vitro parameters.The percent permeation of ZNE through rat skin(ex vivo)from the ethosomal gel was greater(73.12%±1.76%)than that from the conventional gel(38.17%±1.82%).This study reveals the substantial potential of ZNE-loaded ethosomes for transdermal delivery and for use in the management of systemic diseases.展开更多
文摘Zingiber officinale Roscoe(ginger)is traditionally used as a culinary spice worldwide.In folklore medicine,raw and fresh ginger has been used for treating nausea and vomiting,to improve liver function and digestion,antidiarrheal,to treat menstrual cramps,and as an aphrodisiac.Zingerone[4-(4-hydroxy-3-methoxyphenyl)-2-butanone]is the major bioactive ingredient present in ginger.Zingerone has shown a wide-range of pharmacological activities in vitro and in vivo studies.While zingerone is present in small amount in fresh ginger,but its level is increased during drying or heating during cooking.The amount of zingerone increases significantly due to the conversion of gingerol into zingerone through retro-aldol reaction.Owing to its strong antioxidant and anti-inflammatory properties,zingerone has the ability to scavenge reactive oxygen species and to assist in curing a wide array of non-communicable diseases associated with oxidative stress such as diabetes mellitus,obesity,cardiometabolic and cardiovascular disorders,neurological abnormalities,osteoarthritic,and certain cancer types.For this review,extensive literature searches were performed using PubMed,Google Scholar,Science Direct,and other search engines.The major aims of our review are to describe the chemical characteristics of zingerone as well as the various in vitro and in vivo studies reported regarding the pharmacological effects of zingerone and the mechanism of action observed at the cellular and molecular levels.The results of published preclinical and few clinical studies suggest that zingerone has several promising therapeutic applications due to its strong antioxidant,antiinflammatory and anti-proliferative activities without any serious side effects.However,well-designed,randomized,placebo-controlled,and multi-center clinical studies are needed to determine the optimal therapeutic doses,and longterm safety of zingerone.
文摘Transdermal drug delivery offers the benefits of first-pass metabolism avoidance,high bioavailability,a low dose,and high patient compliance.Ethosomes are lipid-based vesicles containing phospholipids,ethanol,and water that enhance drug penetration by overcoming the barrier of the skin.Ethosomes can encapsulate lipophilic as well as hydrophilic drugs to increase their efficacy.Zingerone(ZNE)is a major component found in gingerroot and has potent antidiabetic,antioxidant,and antispasmodic activities.ZNE has low solubility in aqueous media,which leads to low oral bioavailability.ZNE-loaded ethosomes were prepared via the cold method.The ethosomes were optimized by a 3-level and 2-factor full factorial design.The independent variables selected were ethanol(%)and soy lecithin(%).The dependent variables selected were flux(μg/cm^(2)/h)and entrapment efficiency(%).The optimized formulation was evaluated for size,polydispersity index,zeta potential,entrapment efficiency,in vitro drug release,and ex vivo skin drug permeation.The optimized formulation had an average vesicle size of 77.12±1.89 nm,a polydispersity index of 0.350±0.013,a zeta potential of -56.9±1.25 mV,an entrapment efficiency of 75.83%±1.53%,in vitro drug release of 85.97%±1.92%(after 24 h),and ex vivo skin drug permeation of 78.52%±1.62%.The optimized formulation was converted to a gel formulation and characterized for in vitro parameters.The percent permeation of ZNE through rat skin(ex vivo)from the ethosomal gel was greater(73.12%±1.76%)than that from the conventional gel(38.17%±1.82%).This study reveals the substantial potential of ZNE-loaded ethosomes for transdermal delivery and for use in the management of systemic diseases.
