Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy
<b>Background:</b> Acute liver injury (ALI) is a prevalent and potentially lethal condition globally, where pharmacotherapy plays a vital role. However, challenges such as rapid drug excretion and insufficient concentration at hepatic lesions often impede the treatment’s effectiveness. &...
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| author | Yunjie Xu Pinghui Li Shiran Sun Yulin Chen Lixia Feng Dawei Jiang Chidan Wan Jianbo Li Xiong Cai |
| author_facet | Yunjie Xu Pinghui Li Shiran Sun Yulin Chen Lixia Feng Dawei Jiang Chidan Wan Jianbo Li Xiong Cai |
| author_sort | Yunjie Xu |
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| description | <b>Background:</b> Acute liver injury (ALI) is a prevalent and potentially lethal condition globally, where pharmacotherapy plays a vital role. However, challenges such as rapid drug excretion and insufficient concentration at hepatic lesions often impede the treatment’s effectiveness. <b>Methods:</b> We successfully prepared glycyrrhizinate monoammonium cysteine (GMC)-loaded lipid nanoparticles (LNPs) using high-pressure homogenization. The characterization and safety of the LNPs were measured using electrophoretic light scattering (ELS), transmission electron microscopy (TEM), dynamic light scattering (DLS), cytotoxicity assays, and hemolysis tests. The distribution of LNPs in mice was explored using fluorescence labeling methods. The encapsulation efficiency of LNP-GMC was detected using High-Performance Liquid Chromatography (HPLC), and its slow-release effect on GMC was assessed through dialysis. The therapeutic effects of LNP-GMC and pure GMC on the ALI model were evaluated using fibroblast activation protein inhibitor (FAPI) PET imaging, blood biochemical indicators, and liver pathology slices. <b>Results:</b> The encapsulation of GMC in LNPs enhances drug stability and prolongs its hepatic retention, significantly improving its bioavailability and sustained release within the liver. This study also explores the expression of fibroblast activation protein (FAP) in ALI, employing <sup>68</sup>Ga-FAPI PET/CT imaging for effective differentiation and assessment of liver injury. <b>Conclusions:</b> Our results suggest that LNPs offer an enhanced therapeutic approach for ALI treatment, reducing the required drug dosage, and <sup>68</sup>Ga-FAPI PET/CT imaging provides a novel method for diagnosis and treatment assessment. This study contributes valuable insights into the utilization of LNPs in liver disease treatment, presenting a promising direction for future clinical applications. |
| format | Article |
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| institution | Kabale University |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
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| series | Pharmaceutics |
| spelling | doaj-art-2d45101f490144aa8505a68d95385f3e2025-01-24T13:45:55ZengMDPI AGPharmaceutics1999-49232025-01-011719010.3390/pharmaceutics17010090Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury TherapyYunjie Xu0Pinghui Li1Shiran Sun2Yulin Chen3Lixia Feng4Dawei Jiang5Chidan Wan6Jianbo Li7Xiong Cai8Department of Hepatobiliary Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, ChinaThe School of Basic Medical Sciences, Inner Mongolia Medical University, Hohhot 010050, ChinaDepartment of Hepatobiliary Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, ChinaDepartment of Hepatobiliary Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, ChinaDepartment of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, ChinaDepartment of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, ChinaDepartment of Hepatobiliary Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, ChinaDepartment of Nuclear Medicine, The Affiliated Hospital of Inner Mongolia Medical University, Hohhot 010050, ChinaDepartment of Hepatobiliary Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China<b>Background:</b> Acute liver injury (ALI) is a prevalent and potentially lethal condition globally, where pharmacotherapy plays a vital role. However, challenges such as rapid drug excretion and insufficient concentration at hepatic lesions often impede the treatment’s effectiveness. <b>Methods:</b> We successfully prepared glycyrrhizinate monoammonium cysteine (GMC)-loaded lipid nanoparticles (LNPs) using high-pressure homogenization. The characterization and safety of the LNPs were measured using electrophoretic light scattering (ELS), transmission electron microscopy (TEM), dynamic light scattering (DLS), cytotoxicity assays, and hemolysis tests. The distribution of LNPs in mice was explored using fluorescence labeling methods. The encapsulation efficiency of LNP-GMC was detected using High-Performance Liquid Chromatography (HPLC), and its slow-release effect on GMC was assessed through dialysis. The therapeutic effects of LNP-GMC and pure GMC on the ALI model were evaluated using fibroblast activation protein inhibitor (FAPI) PET imaging, blood biochemical indicators, and liver pathology slices. <b>Results:</b> The encapsulation of GMC in LNPs enhances drug stability and prolongs its hepatic retention, significantly improving its bioavailability and sustained release within the liver. This study also explores the expression of fibroblast activation protein (FAP) in ALI, employing <sup>68</sup>Ga-FAPI PET/CT imaging for effective differentiation and assessment of liver injury. <b>Conclusions:</b> Our results suggest that LNPs offer an enhanced therapeutic approach for ALI treatment, reducing the required drug dosage, and <sup>68</sup>Ga-FAPI PET/CT imaging provides a novel method for diagnosis and treatment assessment. This study contributes valuable insights into the utilization of LNPs in liver disease treatment, presenting a promising direction for future clinical applications.https://www.mdpi.com/1999-4923/17/1/90acute liver injurylipid nanoparticlesglycyrrhizinate monoammonium cysteineFAPIPET/CT |
| spellingShingle | Yunjie Xu Pinghui Li Shiran Sun Yulin Chen Lixia Feng Dawei Jiang Chidan Wan Jianbo Li Xiong Cai Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy Pharmaceutics acute liver injury lipid nanoparticles glycyrrhizinate monoammonium cysteine FAPI PET/CT |
| title | Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy |
| title_full | Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy |
| title_fullStr | Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy |
| title_full_unstemmed | Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy |
| title_short | Glycyrrhizinate Monoammonium Cysteine-Loaded Lipid Nanoparticles Allow for Improved Acute Liver Injury Therapy |
| title_sort | glycyrrhizinate monoammonium cysteine loaded lipid nanoparticles allow for improved acute liver injury therapy |
| topic | acute liver injury lipid nanoparticles glycyrrhizinate monoammonium cysteine FAPI PET/CT |
| url | https://www.mdpi.com/1999-4923/17/1/90 |
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