Abstract
Glutathione is a natural anti-aging substance that prevents the oxidation of protein thiols from reactive oxygen species. In the pharmaceutical industry, reduced glutathione (GSH) has been widely used for skin whitening due to its ability to inhibit tyrosinase. However, its poor permeability and foul odor limit its use in skin applications. Herein, we report a GSH-loaded dissolving microneedle (MN) patch prepared with hyaluronic acid (HA) that enables enhanced permeation across the skin and reduces the foul odor of GSH. HA was selected to prepare odorless GSH solutions and used for MN fabrications as a carrier of GSH. GSH-loaded MN (GSH-MN) arrays prepared from MN-forming solution containing up to 10% GSH showed good pattern uniformity and appropriate mechanical properties for insertion into the skin. The GSH-MNs with a loading capacity of 17.4% dissolve within 10 min following insertion into porcine skin and release the loaded GSH without being oxidized. This new approach combines functional biopolymers to reduce the characteristic GSH odor and advanced transdermal delivery based on MN technology to enhance skin permeation without pain. We believe this technique could expand the application of GSH in many cosmeceutical fields.
Highlights
Glutathione, a naturally occurring thiol tripeptide of γ-glutamyl-cysteinyl-glycine, plays a vital role in cellular redox reactions and is involved in the inhibition of melanin synthesis, protection from reactive oxygen species, and cell detoxification [1,2]
The values were found to be less than that of GSH alone (0.59 ± 0.03, 0.75 ± 0.04 and 1.15 ± 0.05 for 1.0 %, 2.5 %, and 5 % of GSH, respectively; Figure 1b). The reason for this result was that the substituted Na+ in hyaluronic acid (HA) reacts with the thiol group of GSH via the reaction formula shown in Supplementary Figure S1
These results show that HA has a better deodorant effect compared to gelatin and Chondroitin sulfate (CS), which is why it was selected for the fabrication of MNs in the present study
Summary
Glutathione, a naturally occurring thiol tripeptide of γ-glutamyl-cysteinyl-glycine, plays a vital role in cellular redox reactions and is involved in the inhibition of melanin synthesis, protection from reactive oxygen species, and cell detoxification [1,2]. Its ability to suppress melanin synthesis through tyrosinase inhibition allows it to be used as a skin whitening agent in cosmeceuticals [5,6,7]. Medicinal peptides are commonly administered by parenteral routes using hypodermic needles. This route requires medical attention for each dose administration and has poor patient compliance due to the pain experienced during injection [12,13]. While topical applications have been used to deliver GSH across the skin, its foul odor and inability to pass through the stratum corneum (SC, the outermost barrier of skin) limit its use [14]
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