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Carica papaya L. belongs to Caricaceae, Brassicales, which is widely distributed in tropical and subtropical areas. In our previous study, the major constituent of C. papaya seeds essential oil was benzyl isothiocyanate (BITC) with a content of up to 99%. It had many advantages such as natural, non-pollution, high purity and strong antifungal activity against Candida strain. However, the application of BITC in pharmaceuticals, food industry and other fields is limited due to its poor aqueous solubility, volatility and easily degradation. In this study, in order to increase the stability and anti-Candida efficacy of BITC, nanostructured lipid carrier loaded with benzyl isothiocyanate from C. papaya seeds (BITC-NLC) was prepared by the melting emulsification ultrasonic method. The physicochemical properties such as morphology, particle size, Zeta potential, encapsulation efficiency, drug loading, etc. were evaluated and its anti-Candida activity was investigated. On the basis of single factor influence test, the orthogonal design was adopted to choose the preparation process of nanostructured lipid carrier (NLC) and formulation of BITC-NLC. The best preparation process was stirring for 20 minutes and ultrasonic dispersion for 15 minutes (amplitude 80%). The best prescription was composed of 50 mg monostearate, 50 mg octyl capric acid triglyceride, 400 mg poloxamer, 400 mg soybean lecithin, 100 mg BITC and 20 mL ultrapure water. The morphology was observed by a transmission electron microscope, the particle size and zeta potential were measured by Zetasizer Nano ZSE, and the encapsulation efficiency and drug loading were analyzed by high performance liquid chromatography. The final prepared BITC-NLC was quasi-spherical shapes and the average particle size, Zeta potential and encapsulation efficiency was 79.13 nm, -21.77 mV and 91.52%, respectively. The preliminary stability test results showed that BITC-NLC was stable for 30 d kept at 25 ℃. The minimal inhibitory concentrations (MICs) were determined using the broth dilution method. MICs of the BITC-NLC against all the selected Candida strains were 8-32 μg/mL, which were better than BITC. In addition, it could inhibit C. albicans and C. tropicalis that are resistant to the most commonly used antifungal drug - fluconazole. The new prepared formulation BITC-NLC from papaya seeds essential oil in this study has small particle size, good physical stability, high encapsulation efficiency and better antifungal effect on C. albicans and C. tropicalis. The results may provide theoretical and experimental basis for the application of papaya seeds which are abundant and typically discarded and the development of natural antifungal drugs.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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