In this study, a stable and highly skin-permeable topical delivery system for itraconazole (ITZ) was designed to provide effective treatment against superficial mycosis. Herein, ITZ was incorporated into a solution composed of ethanol, benzyl alcohol, hydrochloric acid, Transcutol P, and cyclomethicone as a delivery vehicle, solubilizer, protonating agent, permeation enhancer, and spreading agent, respectively. At 72 h, the optimal topical ITZ formulation (ITZ–TF#11) exhibited 135% enhanced skin permeability, which led to increases in drug deposition in the stratum corneum, epidermis, and dermis of 479%, 739%, and 2024%, respectively, compared with the deposition of 1% ITZ in ethanol (control). Moreover, on day 7, ITZ–TF#11 demonstrated 2.09- and 2.30-fold enhanced nail flux and drug deposition, compared with the control. At a dose of 40 mg/kg/day, ITZ–TF#11 showed 323% greater lesion recovery, a 165% lower mean erythema severity score, and a 37% lower mean logarithm of viable fungal cells in skin in the treated area, compared with mice that received oral ITZ at the same dose. Overall, the findings imply that ITZ–TF#11 is a superior alternative to oral ITZ for treatment of superficial mycosis.

In the present study, various extracts of C. tricuspidata fruit were prepared with varying ethanol contents and evaluated for their biomarker and biological properties. The 80% ethanolic extract showed the best tyrosinase inhibitory activity, while the 100% ethanolic extract showed the best total phenolics and flavonoids contents. The HPLC method was applied to analyze the chlorogenic acid in C. tricuspidata fruit extracts. The results suggest that the observed antioxidant and tyrosinase inhibitory activity of C. tricuspidata fruit extract could partially be attributed to the presence of marker compounds in the extract. In this study, we present an analytical method for standardization and optimization of C. tricuspidata fruit preparations. Further investigations are warranted to confirm the in vivo pharmacological activity of C. tricuspidata fruit extract and its active constituents and assess the safe use of the plant for the potential development of the extract as a skin depigmentation agent.

A method for the separation and quantification of acteoside by reverse-phase high-performance liquid chromatography (HPLC) was developed and validated. Hot water and ethanolic extracts of Osmanthus fragrans leaves and flowers were analyzed for acteoside content. Excellent linearity was obtained, with an r2 higher than 0.999. The precision, specificity, and accuracy of our method were excellent, suggesting that it can be conveniently used for the quantification of acteoside in the crude extract of O. fragrans. The hot water and ethanol extracts were analyzed, and their biological activities were tested. The extraction yields, marker (acteoside) contents, and antioxidant activities of the leaf and flower extracts were analyzed. The antioxidant activity was confirmed by measuring the 2,2-diphenyl-2-picrylhydrazyl radical scavenging activity, reducing power, and total phenolic content. The acteoside content tended to be higher in the 100% ethanol extract of O. fragrans compared to those with the other extraction conditions tested. Overall, almost all extracts prepared with ethanolic solvents tended to produce better antioxidant activity than those prepared with hot water. These results suggest that the ethanolic extract of O. fragrans could serve as a potential antioxidant and anti-inflammatory pharmaceutical source, and our validated method would be useful for the quality control of O. fragrans extracts.

Codonopsis lanceolate exerts various medicinal effects and has been used as a traditional medicine for inflammation, asthma, gastritis, and liver disease. Recently, we reported the xanthine oxidase inhibitory activity of C. lanceolata extract and that lobetyolin, one of the key components, was a xanthine oxidase inhibitor. Lobetyolin showed anti-hyperuricemic activity in vitro and in vivo. In this study, we prepared various types of C. lanceolata extracts for the development of functional materials and natural drugs. We present the optimal analytical approach for the quality control and extraction optimization of C. lanceolata preparations. We established and validated a HPLC analysis for easy separation and quantification of the lobetyolin biomarker. Solvent extracts of C. lanceolata root were prepared and the profiles of the active marker and the optimal extraction methods were evaluated. The 100% ethanolic extract demonstrated the highest lobetyolin content. The validated HPLC method confirmed that lobetyolin was present in C. lanceolata root extracts. We suggest that the anti-hyperuricemic activities of C. lanceolata extract could be attributed to this marker compound. The results proposed that the 100% ethanolic extract could be used for the prevention of hyperurecemia, and that this analytical method and biomarker could be useful for the quality control of C. lanceolata preparations.

The purpose of this study was to simultaneously develop anti-hyperuricemic and anti-wrinkle source using Camellia japonica leaf (CJ). CJ extract was prepared. Its contents of biomarkers and biological activities were then analyzed. First, we investigated the extraction efficiency. The extraction rate was 10% or less with hot water or 80% ethanol. HPLC analysis revealed that CJ extract contained rutin, hyperoside, isoquercitrin, chlorogenic acid (CGA), gallocatechin gallate (GCG), and phillygenin. As a result of measuring contents of biomarkers in the extract, CGA was detected in 20, 40, and 60% ethanol extracts. GCG showed the highest content in the hot water extract. Hyperoside and isoquercitrin showed the highest contents in the 80% ethanol extract. Philligenin showed an even content of 0.1% or more in all samples except for 40% ethanol extract. Rutin showed the highest content in 80% ethanol extract. Elastase inhibitory abilities of six extracts and PPRM were investigated at a concentration of 0.5 mg/mL. Results revealed that PPRM and 80% ethanol extract showed about 80% and 62% inhibition, respectively. As a result of comparing elastase inhibitory activities of biomarkers, hyperoside, isoquercitrin, and philligenin showed higher activities. Among six extracts, the extract that could be used as an anti-hyperuricemic source was 80% ethanol extract. When xanthine oxidase (XO) inhibitory activities of biomarkers were evaluated, rutin and hyperoside showed excellent activities. In particular, when XO activity was measured by mixing rutin and hyperoside with 80% ethanol extract, the same efficacy as 80% ethanol extract was obtained. It was predicted that 80% ethanol extract could be used simultaneously as an anti-hyperuricemic and anti-wrinkle source. Further studies are needed to determine anti-hyperuricemic activities of rutin and hyeproside in vivo.