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Abstract
This study aimed to develop nanoemulsions for enhancing chemical stability and dermal delivery of Cordyceps militaris extracts. C. militaris was extracted by maceration and infusion. The extracts were investigated for cordycepin, phenolic, and flavonoid content. The antioxidant activity was investigated by in vitro spectrophotometric methods. The irritation profile was investigated by hen’s egg-chorioallantoic membrane test. Nanoemulsions were developed using high-pressure homogenizer. C. militaris extract was incorporated into the nanoemulsion and investigated for safety, release profile, permeation, and skin retention. The results demonstrated that water extract (CW) contained the significantly highest content of cordycepin, phenolics, and flavonoids, which were responsible for antioxidant activity. CW was the most potent antioxidant. CW possessed comparable 2,2′-diphenyl-1-picrylhydrazyl radical scavenging activity and lipid peroxidation inhibition to l-ascorbic acid (96.9 ± 3.1%) and alpha-tocopherol (87.2 ± 1.0%). Consequently, ten mg/mL of CW was incorporated into nanoemulsions composing of sugar squalene, Tween® 85, and deionized water. Nanoemulsion, which had the smallest internal droplet size (157.1 ± 2.6 nm), enhanced the stability of CW, had no cytotoxicity effect and no skin irritation, released the most CW (0.9 ± 0.0% w/w after 24 h), and delivered the highest CW into the skin layer (33.5 ± 0.7% w/w). Therefore, nanoemulsion was suggested for enhancing the stability and dermal delivery of CW.
Highlights
Cordyceps militaris is a highly valued fungus, which has been used as traditional medicine in China since ancient times [1]
Cordycepin, 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox; purity ≥ 95.0%), l-ascorbic acid, sodium chloride (NaCl), sodium dihydrogen phosphate (NaH2PO4), disodium phosphate (Na2HPO4), sodium phosphate (Na3PO4), sodium carbonate (Na2CO3), sodium thiocyanate (NaSCN), sodium acetate (C2H3NaO2), calcium chloride (CaCl2), ferrous chloride (FeCl2), ferric chloride (FeCl3), ferrous sulfate (FeSO4), potassium persulfate (K2S2O8), hydrochloric acid (HCl), linoleic acid, tricine, tris base, 2,2 -diphenyl-1-picrylhydrazyl reagent (DPPH), 2,2 -azino-bis3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 2,4,6-tripyridyl-striazine (TPTZ), Folin-ciocalteu (FC) reagent, bovine serum albumin (BSA), sodium lauryl sulfate (SLS), sugar squalane, Simmondsia chinensis oil, Argania spinosa oil, polysorbate 20 (Tween® 20), polysorbate 80 (Tween® 80), and polysorbate 85 (Tween® 85) were analytical grade purchased from Sigma-Aldrich
Hexane, ethyl acetate, acetic acid, and dimethyl sulfoxide (DMSO), were analytical grade purchased from Labscan (Dublin, Ireland)
Summary
Cordyceps militaris is a highly valued fungus, which has been used as traditional medicine in China since ancient times [1]. The fruiting bodies of C. militaris have been successfully cultivated on a large-scale and widely used for its health beneficial proprieties all over the world [2]. C. militaris is an edible mushroom, which contains high nutritional and therapeutic value [3]. Cordycepin (3 -deoxyadenosine), an adenosine analogue isolated from C. militaris, has been reported to possess various pharmacological activities, including antioxidant, immunomodulatory, anti-inflammatory, anticarcinogenic, and antiviral agents [3]. It has been extensively studied during the last decade [4,5]
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