Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity

The present study compared the free and encapsulated photosensitizer hypocrellin B (HB) in terms of photophysical-chemical properties, cellular uptake, subcellular distribution, and phototoxicity. The hydrophobic HB was encapsulated into liposomes (HB@Lipo) or poly (lactic-<i data-eusoft-scrollab...

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Main Authors: Weiyan Kang, Feng Zhao, Jixing Cheng, Kaijie Feng, Liang Yan, Yue You, Jinxia Li, Jing Meng
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Nanomaterials
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Online Access:https://www.mdpi.com/2079-4991/15/12/889
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author Weiyan Kang
Feng Zhao
Jixing Cheng
Kaijie Feng
Liang Yan
Yue You
Jinxia Li
Jing Meng
author_facet Weiyan Kang
Feng Zhao
Jixing Cheng
Kaijie Feng
Liang Yan
Yue You
Jinxia Li
Jing Meng
author_sort Weiyan Kang
collection DOAJ
description The present study compared the free and encapsulated photosensitizer hypocrellin B (HB) in terms of photophysical-chemical properties, cellular uptake, subcellular distribution, and phototoxicity. The hydrophobic HB was encapsulated into liposomes (HB@Lipo) or poly (lactic-<i data-eusoft-scrollable-element="1">co</i>-glycolic acid) nanoparticles (HB@PLGA). Encapsulation into nanocarriers exerted no obvious influence on the photophysical-chemical properties of HB, including UV-visible absorbance, fluorescence spectra, singlet oxygen (<sup data-eusoft-scrollable-element="1">1</sup>O<sub data-eusoft-scrollable-element="1">2</sub>) production capacity, and photostability. Free and encapsulated HB revealed some disparities in cellular uptake and subcellular localization patterns. In 2D-cultured B16 cells and tumor spheroids, free HB exhibited the fastest cellular uptake, while HB@PLGA had the lowest, as evidenced. Subcellular localization analysis first revealed a significant colocalization of free HB, HB@Lipo, and HB@PLGA within lipid droplets, with minimal colocalization in mitochondria and the endoplasmic reticulum. Unlike free HB and HB@Lipo, HB@PLGA exhibited strong lysosomal colocalization, indicating a unique intracellular trafficking pathway for PLGA-encapsulated HB. Upon laser irradiation, both free and encapsulated HB induced pronounced phototoxicity with substantial ROS production, confirming the robust PDT effect of HB. The photodynamic killing effect correlated with the intracellular HB content. These findings highlighted the impact of nanoformulation on HB’s cellular behavior and therapeutic performance.
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spelling doaj-art-d827ef82825d48fab5cc26e55b06bb7a2025-08-20T03:27:25ZengMDPI AGNanomaterials2079-49912025-06-01151288910.3390/nano15120889Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and PhototoxicityWeiyan Kang0Feng Zhao1Jixing Cheng2Kaijie Feng3Liang Yan4Yue You5Jinxia Li6Jing Meng7Department of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaLab for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, ChinaLab for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, ChinaLab for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, ChinaLab for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, ChinaLab for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, ChinaLab for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing 100049, ChinaDepartment of Medicinal Chemistry, School of Pharmacy, Hebei Medical University, Shijiazhuang 050017, ChinaThe present study compared the free and encapsulated photosensitizer hypocrellin B (HB) in terms of photophysical-chemical properties, cellular uptake, subcellular distribution, and phototoxicity. The hydrophobic HB was encapsulated into liposomes (HB@Lipo) or poly (lactic-<i data-eusoft-scrollable-element="1">co</i>-glycolic acid) nanoparticles (HB@PLGA). Encapsulation into nanocarriers exerted no obvious influence on the photophysical-chemical properties of HB, including UV-visible absorbance, fluorescence spectra, singlet oxygen (<sup data-eusoft-scrollable-element="1">1</sup>O<sub data-eusoft-scrollable-element="1">2</sub>) production capacity, and photostability. Free and encapsulated HB revealed some disparities in cellular uptake and subcellular localization patterns. In 2D-cultured B16 cells and tumor spheroids, free HB exhibited the fastest cellular uptake, while HB@PLGA had the lowest, as evidenced. Subcellular localization analysis first revealed a significant colocalization of free HB, HB@Lipo, and HB@PLGA within lipid droplets, with minimal colocalization in mitochondria and the endoplasmic reticulum. Unlike free HB and HB@Lipo, HB@PLGA exhibited strong lysosomal colocalization, indicating a unique intracellular trafficking pathway for PLGA-encapsulated HB. Upon laser irradiation, both free and encapsulated HB induced pronounced phototoxicity with substantial ROS production, confirming the robust PDT effect of HB. The photodynamic killing effect correlated with the intracellular HB content. These findings highlighted the impact of nanoformulation on HB’s cellular behavior and therapeutic performance.https://www.mdpi.com/2079-4991/15/12/889hypocrellin BliposomesPLGA nanoparticlescellular uptakesubcellular localizationphotodynamic therapy
spellingShingle Weiyan Kang
Feng Zhao
Jixing Cheng
Kaijie Feng
Liang Yan
Yue You
Jinxia Li
Jing Meng
Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity
Nanomaterials
hypocrellin B
liposomes
PLGA nanoparticles
cellular uptake
subcellular localization
photodynamic therapy
title Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity
title_full Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity
title_fullStr Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity
title_full_unstemmed Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity
title_short Comparative Study of Free and Encapsulated Hypocrellin B on Photophysical-Chemical Properties, Cellular Uptake, Subcellular Distribution, and Phototoxicity
title_sort comparative study of free and encapsulated hypocrellin b on photophysical chemical properties cellular uptake subcellular distribution and phototoxicity
topic hypocrellin B
liposomes
PLGA nanoparticles
cellular uptake
subcellular localization
photodynamic therapy
url https://www.mdpi.com/2079-4991/15/12/889
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