Efficient Delivery and Distribution in Skin of Chlorogenic Acid and Resveratrol Induced by Microemulsion Using Sucrose Laurate

Abstract

To achieve efficient skin delivery of polyphenols, we prepared a novel oil-in-water (o/w)-type microemulsion (MESL) using sucrose laurate as a surfactant and ethanol, isopropyl myristate and water as other components. We examined its usefulness by in vitro studies on skin delivery of chlorogenic acid and resveratrol as hydrophilic and hydrophobic polyphenols using Yucatan micropig skin, and also examined the difference in the distribution of these polyphenols in skin. MESL significantly improved skin incorporation of these polyphenols at all time points examined (6, 20, 40 h) in the epidermis and at 20 and 40 h in the dermis, compared with the microemulsion using Tween 80 as a surfactant component (MEK), although the solubilization capacity of MESL was lower than that of MEK. Using MESL, the incorporation amount in the dermis of each polyphenol increased with time, while the amount in the epidermis was almost constant during the time examined. Incorporation efficiencies into skin of chlorogenic acid and resveratrol induced by MESL at 40 h after application were about 6-fold and 19-fold higher in the epidermis and 3.5-fold and 15-fold higher in the dermis, respectively, than those by MEK. The increase was more prominent for resveratrol. Hydrophilic chlorogenic acid was distributed slightly more in the epidermis, while hydrophobic and smaller-molecularweight resveratrol was mainly distributed in the dermis. These findings suggest that MESL could be a promising vehicle for the efficient skin delivery of chlorogenic acid and resveratrol, especially for resveratrol to the dermis.Key words microemulsion; sucrose laurate; polyphenol; chlorogenic acid; resveratrol; skin Polyphenols are well-known antioxidants and have been shown to have a wide range of therapeutic potential, such as via anti-inflammatory and anticancer activities, as well as protective effects against cardiovascular and neurodegenerative diseases.1,2) Polyphenols can also be applied to skin for topical effects, including protection against UV-induced oxidative damage (photoaging), skin cancer prevention and skin care 3,4) ; however, the penetration of polyphenols into skin is often limited due to their poor solubility in both aqueous and organic solvents as well as relatively high molecular weight. There is thus a need for enhancement systems to be introduced for their topical application.Microemulsions consist of an aqueous phase, an oil phase, a surfactant and a co-surfactant component, which are thermodynamically stable and have been shown to have high solubilization capacity and to facilitate the skin incorporation of both hydrophilic and lipophilic drugs. 5,6) In previous studies, we revealed that microemulsions using polyoxyethylene sorbitan monooleate (Tween 80) as a surfactant component are useful for the intradermal delivery of polyphenols, such as quercetin, genistein and chlorogenic acid. 7-9) However, the incorporation efficiencies of these polyphenols from the vehicle into skin were low. In another study, we also revealed that an anionic su...

Polyphenols as active ingredients for cosmetic products

“…The smallest and the most hydrophilic protocatechuic acid exhibited the highest permeation rates, followed by catechin, resveratrol, rutin, quercetin and EGCG, respectively. Similarly, after the in vitro permeation study using guinea pig skin and Yucatan micropig skin, hydrophobic resveratrol with its smaller molecular weight was mainly distributed in the dermis, whereas hydrophilic chlorogenic acid was found more in the epidermis [84]. Similar findings were obtained in other studies.…”

“…The formulation of hydrophobic quercetin to a W/O-microemulsion, however, considerably improved the intradermal delivery; quercetin penetrated into deeper skin layers [88]. The incorporation of chlorogenic acid, resveratrol, curcumin and quercetin to O/W microemulsions, containing sucrose laurate or di-2-ethylhexyl sodium sulfosuccinate, could enhance the delivery of these polyphenols into the dermis in vitro in comparison with the microemulsions containing Tween 80 (polyoxyethylenesorbitan monooleate) [84,90]. The incorporation of chlorogenic acid, resveratrol, curcumin and quercetin to O/W microemulsions, containing sucrose laurate or di-2-ethylhexyl sodium sulfosuccinate, could enhance the delivery of these polyphenols into the dermis in vitro in comparison with the microemulsions containing Tween 80 (polyoxyethylenesorbitan monooleate) [84,90].…”

Prominent efficiency in skin delivery of resveratrol by novel sucrose oleate microemulsion

“…In vitro studies on the intradermal and transdermal delivery of resveratrol were performed as described previously . YMP skin was mounted in a Franz‐type diffusion cell with a water jacket (37 °C).…”

“…Sucrose fatty acid esters are well known as biodegradable non‐ionic surfactants consisting of hydrophilic sucrose and lipophilic fatty acids, which are non‐toxic, non‐sensitizing, cause no skin irritation and have been applied in many fields, such as the food, cosmetic and pharmaceutical industries . In a recent study, we clarified that water‐rich microemulsion consisting of sucrose laurate as a surfactant component and ethanol, isopropyl myristate (IPM) and water as other components (MESL) was highly effective for the intradermal delivery of resveratrol and chlorogenic acid compared with microemulsion using Tween 80 as a surfactant component …”

ImprovingIn VivoEfficacy of Bioactive Molecules: An Overview of Potentially Antitumor Phytochemicals and Currently Available Lipid-Based Delivery Systems

“…For topical application, the incorporation of active compounds into nanocarriers aims to enhance skin permeation and stability, lengthen systemic circulating time, and minimize metabolic degradation and systemic toxicity. Thus, for instance, MEs provide a safe, effective, and noninvasive means to topically deliver Phy such as quercetin [158], genistein [159], and chlorogenic acid and resveratrol [160]. Other nanocarriers used for the topical delivery of Phy include liposomes, ethosomes, NLCs, polymeric NPs, and polymer-bioactive conjugates (Table 6).…”