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β-lapachone nanostructured lipid carriers: repolarization of tumor-associated macrophages for osteosarcoma therapy.

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Title: β-lapachone nanostructured lipid carriers: repolarization of tumor-associated macrophages for osteosarcoma therapy.
Authors: Martínez-Borrajo, Rebeca1, Lorenzo-Lorenzo, Arturo Alejandro1, Landin, Mariana1 m.landin@usc.es, Díaz-Rodríguez, Patricia1 patricia.diaz.rodriguez@usc.es
Source: Journal of Osteoporosis & Mineral Metabolism / Revista de Osteoporosis y Metabolismo Mineral (Spanish edition). jul-sep2025, Vol. 17 Issue 3, p117-127. 11p.
Subjects: OSTEOSARCOMA, MACROPHAGES, NAPHTHOQUINONE, CANCER treatment, MACROPHAGE activation, DRUG delivery systems
Abstract: Osteosarcoma (OS) is the most common primary malignant bone tumor. Tumor-associated macrophages (TAMs) represent up to 50 % of the cells in the tumor and play a significant role in tumor metastasis and tumoral immunosuppression. The modification of TAMs phenotype has been identified as suitable for controlling tumor progression. Nanoparticles are versatile drug delivery systems that allow enhanced drug tumor accumulation through passive and active targeting. Among NPs, nanostructured lipid carriers (NLCs) possess a unique imperfect matrix structure with increased drug loading capacity of highly hydrophobic drugs. ß-Lapachone (ß-Lap) is a natural naphthoquinone with anti-tumor activity against various cancer cells. The aim of this work is to design and optimize a NLCs formulation loaded with ß-Lapachone to be specifically internalized by TAMs for OS treatment. This approach will use hybrid artificial intelligence tools to functionalize the NLCs with the CD206 ligand mannose. To optimize NLCs preparation, various liquid and solid lipids were tested for drug solubility. AI tools were employed to design NLCs with desired properties, resulting in formulations with particle sizes < 100 nm and stable physicochemical properties. Mannose functionalization enhanced macrophage internalization of the NLCs. Moreover, in vitro studies demonstrated these NLCs, particularly the mannose-functionalized formulation, induced a further pro-inflammatory M1-like polarization in TAMs, evidenced by increased TNF-a and IL-6 secretion. This TAMs polarization strategy, combined with the localized delivery of ß-Lap, offers a promising approach for OS therapy. [ABSTRACT FROM AUTHOR]
Copyright of Journal of Osteoporosis & Mineral Metabolism / Revista de Osteoporosis y Metabolismo Mineral (Spanish edition) is the property of Ibanez y Plaza and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Database: MedicLatina
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  Data: β-lapachone nanostructured lipid carriers: repolarization of tumor-associated macrophages for osteosarcoma therapy.
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  Data: &lt;searchLink fieldCode=&quot;AR&quot; term=&quot;%22Mart&#237;nez-Borrajo%2C+Rebeca%22&quot;&gt;Mart&#237;nez-Borrajo, Rebeca&lt;/searchLink&gt;&lt;relatesTo&gt;1&lt;/relatesTo&gt;&lt;br /&gt;&lt;searchLink fieldCode=&quot;AR&quot; term=&quot;%22Lorenzo-Lorenzo%2C+Arturo+Alejandro%22&quot;&gt;Lorenzo-Lorenzo, Arturo Alejandro&lt;/searchLink&gt;&lt;relatesTo&gt;1&lt;/relatesTo&gt;&lt;br /&gt;&lt;searchLink fieldCode=&quot;AR&quot; term=&quot;%22Landin%2C+Mariana%22&quot;&gt;Landin, Mariana&lt;/searchLink&gt;&lt;relatesTo&gt;1&lt;/relatesTo&gt;&lt;i&gt; m.landin@usc.es&lt;/i&gt;&lt;br /&gt;&lt;searchLink fieldCode=&quot;AR&quot; term=&quot;%22D&#237;az-Rodr&#237;guez%2C+Patricia%22&quot;&gt;D&#237;az-Rodr&#237;guez, Patricia&lt;/searchLink&gt;&lt;relatesTo&gt;1&lt;/relatesTo&gt;&lt;i&gt; patricia.diaz.rodriguez@usc.es&lt;/i&gt;
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  Data: Osteosarcoma (OS) is the most common primary malignant bone tumor. Tumor-associated macrophages (TAMs) represent up to 50 % of the cells in the tumor and play a significant role in tumor metastasis and tumoral immunosuppression. The modification of TAMs phenotype has been identified as suitable for controlling tumor progression. Nanoparticles are versatile drug delivery systems that allow enhanced drug tumor accumulation through passive and active targeting. Among NPs, nanostructured lipid carriers (NLCs) possess a unique imperfect matrix structure with increased drug loading capacity of highly hydrophobic drugs. &#223;-Lapachone (&#223;-Lap) is a natural naphthoquinone with anti-tumor activity against various cancer cells. The aim of this work is to design and optimize a NLCs formulation loaded with &#223;-Lapachone to be specifically internalized by TAMs for OS treatment. This approach will use hybrid artificial intelligence tools to functionalize the NLCs with the CD206 ligand mannose. To optimize NLCs preparation, various liquid and solid lipids were tested for drug solubility. AI tools were employed to design NLCs with desired properties, resulting in formulations with particle sizes &lt; 100 nm and stable physicochemical properties. Mannose functionalization enhanced macrophage internalization of the NLCs. Moreover, in vitro studies demonstrated these NLCs, particularly the mannose-functionalized formulation, induced a further pro-inflammatory M1-like polarization in TAMs, evidenced by increased TNF-a and IL-6 secretion. This TAMs polarization strategy, combined with the localized delivery of &#223;-Lap, offers a promising approach for OS therapy. [ABSTRACT FROM AUTHOR]
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  Data: &lt;i&gt;Copyright of Journal of Osteoporosis &amp; Mineral Metabolism / Revista de Osteoporosis y Metabolismo Mineral (Spanish edition) is the property of Ibanez y Plaza and its content may not be copied or emailed to multiple sites without the copyright holder&#39;s express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.&lt;/i&gt; (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
  BibEntity:
    Identifiers:
      – Type: doi
        Value: 10.20960/RevOsteoporosMetabMiner.00082
    Languages:
      – Code: eng
        Text: English
    PhysicalDescription:
      Pagination:
        PageCount: 11
        StartPage: 117
    Subjects:
      – SubjectFull: OSTEOSARCOMA
        Type: general
      – SubjectFull: MACROPHAGES
        Type: general
      – SubjectFull: NAPHTHOQUINONE
        Type: general
      – SubjectFull: CANCER treatment
        Type: general
      – SubjectFull: MACROPHAGE activation
        Type: general
      – SubjectFull: DRUG delivery systems
        Type: general
    Titles:
      – TitleFull: β-lapachone nanostructured lipid carriers: repolarization of tumor-associated macrophages for osteosarcoma therapy.
        Type: main
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            NameFull: Martínez-Borrajo, Rebeca
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            NameFull: Lorenzo-Lorenzo, Arturo Alejandro
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            NameFull: Landin, Mariana
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            NameFull: Díaz-Rodríguez, Patricia
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          Dates:
            – D: 01
              M: 07
              Text: jul-sep2025
              Type: published
              Y: 2025
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            – TitleFull: Journal of Osteoporosis & Mineral Metabolism / Revista de Osteoporosis y Metabolismo Mineral (Spanish edition)
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