Abstract
Dermal aging is characterized by states of oxidative stress, chronic inflammation, and abnormal proteolytic degradation due to the action of hydrogen peroxide, superoxide, 5-lipoxygenase, and elastase, respectively. Noteworthy elastase inhibition has previously been reported, and so this study aimed to investigate the ability of Myrsine africana and myrsinoside B to reduce the activity of hydrogen peroxide, superoxide, and 5-lipoxygenase as supplementary mechanisms of action by which M. africana may reduce the appearance of wrinkles. The use of maltose microneedles were also investigated as a means to enhance the delivery of myrsinoside B into the skin as this is a crucial aspect to investigate when characterizing the efficacy of an active ingredient. Myrsine africana has traditionally been used for skin allergies, boils, and to purify blood (as an astringent) and was selected for this study based on it use in skincare. The crude extract exhibited IC50’s of 56.08 ± 2.88 and 132.74 ± 1.64 µg/ml against the hydrogen peroxide and superoxide radicals, while myrsinoside B exhibited IC50’s of 52.19 ± 4.16 and 192.14 ± 3.52 µg/ml, respectively. The IC50 of the extract and compound against 5-lipoxygenase was 29.65 ± 2.92 and 29.33 ± 3.08 µg/ml, respectively. No toxicity was observed in vitro at the highest concentration tested. Microneedle treatment increased the permeation of the active through the skin after 24 h to 12.46 ± 5.14 µg/cm2 compared to the passive group (1.30± 0.85 µg/cm2). The amount of active retained in the epidermis and dermis was 8.97 ± 0.90 and 6.98 ± 0.73 µg/cm2 respectively, greater than the retention observed in the passive group (3.24 ± 1.41 and 3.27 ± 1.47 µg/cm2, respectively). M. africana and myrsinoside B showed promising antioxidant and anti-inflammatory activity thus supporting the potential of M. africana and myrsinoside B as anti-wrinkle agents. Further, treatment of dermatomed human skin with maltose microneedles facilitated topical delivery of myrsinoside B and provided an effective means for compound delivery to ensure maximum effect.
Highlights
The science of aging skin has long been a topic of interest with the demand for effective botanical actives a particular area of curiosity
The M. africana ethanolic extract scavenged 50% of the superoxide radical at a concentration of 132.74 ± 1.64 μg/ ml, significantly lower than the IC50 of Myrsinoside B (192.14± 3.34 μg/ml), but significantly higher than the positive drug control quercetin (15.29 ± 3.68 μg/ml) (p < 0.01) (Table 1)
The results indicate that both the crude extract of M. africana and myrsinoside B showed inhibition of 5-LOX, with IC50’s of 29.65 ± 2.92 and 29.23 ± 3.08 μg/ml respectively, not significantly different from one another, but significantly higher (p < 0.01) than caffeic acid (14.87 ± 0.69 μg/ml) (Table 1)
Summary
The science of aging skin has long been a topic of interest with the demand for effective botanical actives a particular area of curiosity. Hydrogen peroxide and superoxide are produced in this process and interact undesirably with biological molecules to enhance the activity of proteases such as elastase which proceed to degrade structural components. Inflammatory enzymes such as 5-lipoxygenase are recruited to the affected site and further elicit a stress response. The ability of biologically active molecules to penetrate the skin is significant to ensure delivery to the targeted site. Microneedles are actively employed in the cosmetic industry and are even available for home use, making their potential promising (Bhatnagar et al, 2017)
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