热带作物学报

番木瓜籽挥发油纳米结构脂质载体的制备及抗假丝酵母菌活性研究

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姚凯 ¹^,² , 马寅正 ¹^,³ , 易国辉 ¹ , 王元晓 ¹^,² , 周霞 ¹^,² , 臧旭 ¹^,² , 刘禹棋 ¹^,² , 汪桐 ¹^,² , 何小稳 ¹^,⁴^,^*

热带作物学报 | 采后处理与质量安全 2023,44(7): 1478-1487

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热带作物学报 | 采后处理与质量安全 2023, 44(7): 1478-1487

番木瓜籽挥发油纳米结构脂质载体的制备及抗假丝酵母菌活性研究

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姚凯¹^,², 马寅正¹^,³, 易国辉¹, 王元晓¹^,², 周霞¹^,², 臧旭¹^,², 刘禹棋¹^,², 汪桐¹^,², 何小稳¹^,⁴^,^*

作者信息

^1.海南医学院科学实验中心，海南海口　571199

^2.海南医学院药学院，海南海口　571199

^3.海南医学院公共卫生与全健康国际学院，海南海口　571199

^4.海南省热带心血管病研究重点实验室，海南海口　571199

姚凯（1999—），男，本科生，研究方向：天然植物成分的研究与应用。

通讯作者:

^* 何小稳（HE Xiaowen），E-mail: xiaowen_he@126.com。

Preparation of Nanostructured Lipid Carrier Loaded with Carica papaya Seeds Essential Oil and Its Anti-Candida Activity

Kai YAO¹^,², Yinzheng MA¹^,³, Guohui YI¹, Yuanxiao WANG¹^,², Xia ZHOU¹^,², Xu ZANG¹^,², Yuqi LIU¹^,², Tong WANG¹^,², Xiaowen HE¹^,⁴^,^*

Affiliations

^1.Public Research Center, Hainan Medical University, Haikou, Hainan 571199, China

^2.School of Pharmacy, Hainan Medical University, Haikou, Hainan 571199, China

^3.International School of Public Health and One Health, Hainan Medical University, Haikou, Hainan 571199, China

^4.Key Laboratory of Tropical Cardiovascular Diseases Research of Hainan Province, Haikou, Hainan 571199, China

出版时间: 2023-07-25 doi: 10.3969/j.issn.1000-2561.2023.07.019

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摘要

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番木瓜（Carica papaya Linn.）属十字花目番木瓜科，广泛分布于热带、亚热带地区。课题组前期研究发现，番木瓜籽挥发油的主成分为异硫氰酸苄酯（BITC），含量高达99%，具有天然、无污染、纯度高等特点，且对多种假丝酵母菌均具有明显的抑制作用。但由于BITC水溶性差、易挥发、易降解等缺点，限制了其应用。本研究采用熔融乳化超声法制备异硫氰酸苄酯纳米结构脂质载体（BITC-NLC），并进行形态、粒径及Zeta电位、包封率、载药量等方面的表征及其抗假丝酵母菌活性研究，旨在提高BITC的稳定性和抑菌效果。在单因素试验基础上通过正交试验设计，优化纳米结构脂质载体（NLC）的制备工艺和BITC-NLC的处方组成，得到最佳制备工艺：初乳搅拌20 min，超声分散15 min（振幅80%）；最佳处方组成：单硬脂酸甘油酯50 mg，辛癸酸三甘油酯 50 mg，聚醚F188 400 mg，大豆卵磷脂400 mg，BITC 100 mg，蒸馏水20 mL。采用透射电子显微镜观察形态，纳米粒度及Zeta电位测定仪测定粒径及Zeta电位，高效液相色谱法测定包封率和载药量。最终制备得到的BITC-NLC呈类球形，平均粒径为79.13 nm，Zeta电位为-21.77 mV，包封率为91.52%。初步稳定性试验结果显示，BITC-NLC在25 ℃下贮存30 d的稳定性良好。采用微量稀释法测得制剂对供试白假丝酵母菌（Candida albicans）和热带假丝酵母菌（C. tropicalis）的最低抑菌浓度（MIC）为8~32 μg/mL，比原料药BITC的抑菌效果好，且对耐药菌株也具有抑菌效果。综上，本研究制备的番木瓜籽挥发油新剂型BITC-NLC粒径小，稳定性好，包封率高，对假丝酵母菌抑制作用强，为大量存在且多被丢弃的番木瓜籽的合理开发和综合应用提供依据。

关键词

番木瓜籽 / 挥发油 / 异硫氰酸苄酯 / 纳米结构脂质载体 / 假丝酵母菌

Abstract

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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.

Key words

papaya seeds / essential oil / benzyl isothiocyanate / nanostructured lipid carrier / Candida

引用本文

姚凯, 马寅正, 易国辉, 王元晓, 周霞, 臧旭, 刘禹棋, 汪桐, 何小稳. 番木瓜籽挥发油纳米结构脂质载体的制备及抗假丝酵母菌活性研究. 热带作物学报, 2023 , 44 (7) : 1478 -1487 . DOI: 10.3969/j.issn.1000-2561.2023.07.019

Kai YAO, Yinzheng MA, Guohui YI, Yuanxiao WANG, Xia ZHOU, Xu ZANG, Yuqi LIU, Tong WANG, Xiaowen HE. Preparation of Nanostructured Lipid Carrier Loaded with Carica papaya Seeds Essential Oil and Its Anti-Candida Activity[J]. Chinese Journal of Tropical Crops, 2023 , 44 (7) : 1478 -1487 . DOI: 10.3969/j.issn.1000-2561.2023.07.019

基金

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海南省基础与应用基础研究计划（自然科学领域）高层次人才项目(2019RC219)
海南医学院大学生创新创业训练计划项目(X202211810034)
国家级大学生创新创业训练计划项目(202111810005)

参考文献

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2023年第44卷第7期

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文章信息

doi: 10.3969/j.issn.1000-2561.2023.07.019

接收时间：2022-06-07
首发时间：2026-03-05
出版时间：2023-07-25

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收稿日期：2022-06-07
修回日期：2022-09-15

基金

海南省基础与应用基础研究计划（自然科学领域）高层次人才项目(2019RC219)

海南医学院大学生创新创业训练计划项目(X202211810034)

国家级大学生创新创业训练计划项目(202111810005)

作者信息

^1.海南医学院科学实验中心，海南海口　571199

^2.海南医学院药学院，海南海口　571199

^3.海南医学院公共卫生与全健康国际学院，海南海口　571199

^4.海南省热带心血管病研究重点实验室，海南海口　571199

通讯作者:

^* 何小稳（HE Xiaowen），E-mail: xiaowen_he@126.com。

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https://castjournals.cast.org.cn/joweb/rdzwxb/CN/10.3969/j.issn.1000-2561.2023.07.019

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2种不同金属材料的力学参数

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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