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

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Bibliographic Details
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]
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Database:	MedicLatina

Description
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]
ISSN:	1889836X
DOI:	10.20960/RevOsteoporosMetabMiner.00082