Transcutaneous permeation of topically applied materials is usually blocked by the formidable barrier property of stratum corneum, as the outermost layer of skin. As a result, commonly used cosmetic ingredients cannot easily reach their site of actions. α-bisabolol is a well-known skin whitening ag...
Transcutaneous permeation of topically applied materials is usually blocked by the formidable barrier property of stratum corneum, as the outermost layer of skin. As a result, commonly used cosmetic ingredients cannot easily reach their site of actions. α-bisabolol is a well-known skin whitening agent, whose mechanism of action is by inhibiting the α-melanocyte stimulating hormone (α-MSH) -induced melanogenesis by suppressing cAMP response element binding protein (CREB) phosphorylation. Based on the working mechanism, α-MSH has to reach basal layer to be effective. In this study, using α-bisabolol as a the model compound, the change of permeation profile of model compound by using multi-lamellar emulsion (MLE) as a vehicle was investigated. MLE is a physiologic lipid mixture, comprised with major human stratum corneum (SC) intercellular lipids, ceramide, free fatty acids, and cholesterol. The structural property of test formula was assessed by cross-polarized microscope, phase stability and other physical properties were also measured. The effects of oil types, hydrophilic-lipophilic balance (HLB) value of emulsifiers, dosage of ethanol and α-bisabolol, types of enhancers, usage of viscosity modifying agent, and oil contents on the formation of lamellar structure and other physical properties, as well as the permeation of α-bisabolol were investigated. As results, triglyceride type oil (capric/caprylic triglyceride), and emulsifiers of HLB value of 9 to 12 increased the permeation of topically applied α-bisabolol. Polysorbate 80, as a permeation enhancer, also increased the permeation. Use of carbomer, as a viscosity modifying agent, did not change the permeation property but improved the stability of the formula through increasing the viscosity. Interestingly, formation of lamellar structure was positively correlated with the permeation of test compound. Based on these results, the optimal formula was selected based on the formation of lamellar structure and permeation properties and its clinical efficacy was assessed. Skin whitening effect of selected formulat was observed in clinical study, which confirms the hypothesis. As a conclusion, these results suggest that the lamellar structure forming ability of topical vehicle is positively correlated with the transcutaneous permeation of target molecules.
Transcutaneous permeation of topically applied materials is usually blocked by the formidable barrier property of stratum corneum, as the outermost layer of skin. As a result, commonly used cosmetic ingredients cannot easily reach their site of actions. α-bisabolol is a well-known skin whitening agent, whose mechanism of action is by inhibiting the α-melanocyte stimulating hormone (α-MSH) -induced melanogenesis by suppressing cAMP response element binding protein (CREB) phosphorylation. Based on the working mechanism, α-MSH has to reach basal layer to be effective. In this study, using α-bisabolol as a the model compound, the change of permeation profile of model compound by using multi-lamellar emulsion (MLE) as a vehicle was investigated. MLE is a physiologic lipid mixture, comprised with major human stratum corneum (SC) intercellular lipids, ceramide, free fatty acids, and cholesterol. The structural property of test formula was assessed by cross-polarized microscope, phase stability and other physical properties were also measured. The effects of oil types, hydrophilic-lipophilic balance (HLB) value of emulsifiers, dosage of ethanol and α-bisabolol, types of enhancers, usage of viscosity modifying agent, and oil contents on the formation of lamellar structure and other physical properties, as well as the permeation of α-bisabolol were investigated. As results, triglyceride type oil (capric/caprylic triglyceride), and emulsifiers of HLB value of 9 to 12 increased the permeation of topically applied α-bisabolol. Polysorbate 80, as a permeation enhancer, also increased the permeation. Use of carbomer, as a viscosity modifying agent, did not change the permeation property but improved the stability of the formula through increasing the viscosity. Interestingly, formation of lamellar structure was positively correlated with the permeation of test compound. Based on these results, the optimal formula was selected based on the formation of lamellar structure and permeation properties and its clinical efficacy was assessed. Skin whitening effect of selected formulat was observed in clinical study, which confirms the hypothesis. As a conclusion, these results suggest that the lamellar structure forming ability of topical vehicle is positively correlated with the transcutaneous permeation of target molecules.
주제어
#Multi lamella emulsion (MLE)
#α-Bisabolol
#Topical delivery
#Stratum corneum
#Drug delivery system
#Hydrophilic-lipophilic balance
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