Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds

Candida albicans is the most prominent conditional fungal pathogen, which can cause systemic candidiasis when an individual becomes immunocompromised. The widespread and long-term use of azoles like fluconazole (FLC) has led to a significant increase in drug resistance, posing substantial challenges...

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Main Authors: Zelin Zheng, Zijie Li, Mingqi Yu, Xinyi Ma, Jie Gao, Yan Wang, Jinyan Wu, Xiaodan Yu, Yinzheng Ma, Xiaowen He
Format: Article
Language:English
Published: Taylor & Francis Group 2025-12-01
Series:Drug Delivery
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Online Access:https://www.tandfonline.com/doi/10.1080/10717544.2025.2544687
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author Zelin Zheng
Zijie Li
Mingqi Yu
Xinyi Ma
Jie Gao
Yan Wang
Jinyan Wu
Xiaodan Yu
Yinzheng Ma
Xiaowen He
author_facet Zelin Zheng
Zijie Li
Mingqi Yu
Xinyi Ma
Jie Gao
Yan Wang
Jinyan Wu
Xiaodan Yu
Yinzheng Ma
Xiaowen He
author_sort Zelin Zheng
collection DOAJ
description Candida albicans is the most prominent conditional fungal pathogen, which can cause systemic candidiasis when an individual becomes immunocompromised. The widespread and long-term use of azoles like fluconazole (FLC) has led to a significant increase in drug resistance, posing substantial challenges to clinical treatment. In our previous study, benzyl isothiocyanate (BITC) was extracted from Carica papaya L. seed, and it exhibited a notable inhibitory effect against C. albicans. However, the application of BITC is restricted by its instability, poor water solubility, volatility, and easy degradation. This study aimed to prepare BITC-loaded nanostructured lipid carrier (BITC-NLC) to address these limitations of BITC and enhance antifungal efficacy in vitro and in vivo against C. albicans. The results of physicochemical properties showed that BITC-NLC had small particle size, good physical stability, and high encapsulation efficiency. In vitro, the antifungal effect of BITC-NLC was better than BITC against both sensitive and resistant C. albicans and better than FLC against resistant C. albicans. Moreover, in the in vivo experiment using systemic candidiasis mice model induced by resistant C. albicans, BITC-NLC was more remarkable than BITC and FLC in the increase of the survival rate and the splenic index, the reduction of the fungal burden, and the alleviation of the pathological damage. These findings may be attributed to the enhanced stability and sustained release of BITC. This study highlights the potential of BITC-NLC as a novel and effective formulation for the clinical treatment of drug-resistant C. albicans infections, thereby expanding the application scope of papaya.
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spelling doaj-art-54eabe9a7ddb4552aeee4499c07b23512025-08-20T03:36:10ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642025-12-0132110.1080/10717544.2025.2544687Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seedsZelin Zheng0Zijie Li1Mingqi Yu2Xinyi Ma3Jie Gao4Yan Wang5Jinyan Wu6Xiaodan Yu7Yinzheng Ma8Xiaowen He9School of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaSchool of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaSchool of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaSchool of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaSchool of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaResearch Institute for Science and Technology Development, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaResearch Institute for Science and Technology Development, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaResearch Institute for Science and Technology Development, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaSchool of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaSchool of Pharmacy, Hainan Medical University (Hainan Academy of Medical Sciences), Haikou, ChinaCandida albicans is the most prominent conditional fungal pathogen, which can cause systemic candidiasis when an individual becomes immunocompromised. The widespread and long-term use of azoles like fluconazole (FLC) has led to a significant increase in drug resistance, posing substantial challenges to clinical treatment. In our previous study, benzyl isothiocyanate (BITC) was extracted from Carica papaya L. seed, and it exhibited a notable inhibitory effect against C. albicans. However, the application of BITC is restricted by its instability, poor water solubility, volatility, and easy degradation. This study aimed to prepare BITC-loaded nanostructured lipid carrier (BITC-NLC) to address these limitations of BITC and enhance antifungal efficacy in vitro and in vivo against C. albicans. The results of physicochemical properties showed that BITC-NLC had small particle size, good physical stability, and high encapsulation efficiency. In vitro, the antifungal effect of BITC-NLC was better than BITC against both sensitive and resistant C. albicans and better than FLC against resistant C. albicans. Moreover, in the in vivo experiment using systemic candidiasis mice model induced by resistant C. albicans, BITC-NLC was more remarkable than BITC and FLC in the increase of the survival rate and the splenic index, the reduction of the fungal burden, and the alleviation of the pathological damage. These findings may be attributed to the enhanced stability and sustained release of BITC. This study highlights the potential of BITC-NLC as a novel and effective formulation for the clinical treatment of drug-resistant C. albicans infections, thereby expanding the application scope of papaya.https://www.tandfonline.com/doi/10.1080/10717544.2025.2544687Papaya seedsbenzyl isothiocyanatenanostructured lipid carrierCandida albicansresistancesystemic candidiasis
spellingShingle Zelin Zheng
Zijie Li
Mingqi Yu
Xinyi Ma
Jie Gao
Yan Wang
Jinyan Wu
Xiaodan Yu
Yinzheng Ma
Xiaowen He
Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds
Drug Delivery
Papaya seeds
benzyl isothiocyanate
nanostructured lipid carrier
Candida albicans
resistance
systemic candidiasis
title Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds
title_full Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds
title_fullStr Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds
title_full_unstemmed Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds
title_short Enhanced in vitro and in vivo antifungal efficacy against Candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from Carica papaya L. seeds
title_sort enhanced in vitro and in vivo antifungal efficacy against candida albicans of nanostructured lipid carrier loaded with benzyl isothiocyanate extracted from carica papaya l seeds
topic Papaya seeds
benzyl isothiocyanate
nanostructured lipid carrier
Candida albicans
resistance
systemic candidiasis
url https://www.tandfonline.com/doi/10.1080/10717544.2025.2544687
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