Targeted deoxycholic acid-loaded nanoliposomes enhance cell-associated uptake and modulate polarization-associated markers in THP-1-derived M2-like macrophages
Abstract
Tumor-associated macrophages (TAMs) frequently exhibit M2-like properties that support tumor progression. Deoxycholic acid (DCA), a secondary bile acid with amphiphilic membrane activity and context-dependent immunomodulatory effects, may influence macrophage phenotype. This study developed mannose-targeted DCA-loaded nanoliposomes and evaluated their physicochemical characteristics, cell-associated uptake, cytotoxicity, and effects on polarization-associated markers in THP-1-derived M2-like macrophages. Cellular uptake was assessed qualitatively by DiI fluorescence microscopy in two replicate experiments. Cytotoxicity was evaluated by MTT assay over 0.25-100 µM, and CD80/CD206 expression was assessed by flow cytometry after exposure to 10 or 20 µM DCA for 48 h. The targeted formulation had a mean hydrodynamic diameter of 155.1 ± 0.34 nm, a PDI of 0.28, a zeta potential of -12.8 ± 0.6 mV, spherical morphology, and an encapsulation efficiency of 82.94%. HPLC showed a DCA-associated peak at 6.215 min in the reference standard, disrupted DCA-loaded liposomes, and the unencapsulated fraction, whereas no corresponding peak was detected in the mobile-phase or blank-liposome controls. The formulation produced concentration-dependent cytotoxicity, with an estimated IC ₅₀ of 13.47 µM. At 20 µM for 48 h, the percentage of CD206-positive cells changed from 76.8 ± 2.31% to 21.7 ± 1.98%, whereas the percentage of CD80-positive cells changed from 18.6 ± 1.72% to 68.3 ± 2.54%. Because 20 µM exceeded the estimated IC ₅₀ , these observations may partly reflect selective cell loss. Flow-cytometric measurements were performed in triplicate (n = 3), but confirmation in independent biological experiments remains necessary. Additional viability-matched and functionally validated experiments are required.
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BibTeX
@article{darmanto2026targeted,
title = {{Targeted deoxycholic acid-loaded nanoliposomes enhance cell-associated uptake and modulate polarization-associated markers in THP-1-derived M2-like macrophages}},
author = {Win Darmanto and Sri Puji Astuti Wahyuningsih and Firli Rahmah Primula Dewi and Ally Kafesa and Mochammad Aqilah Herdiansyah and Rr.Aulia Rahmawati Kusuma Putri and Liew Kai Bin and Intan Zarina Zainol Abidin},
journal = {Scientific Reports},
year = {2026},
month = oct,
doi = {10.1038/s41598-026-73503-w},
url = {https://www.nature.com/articles/s41598-026-73503-w},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Targeted deoxycholic acid-loaded nanoliposomes enhance cell-associated uptake and modulate polarization-associated markers in THP-1-derived M2-like macrophages
AU - Win Darmanto
AU - Sri Puji Astuti Wahyuningsih
AU - Firli Rahmah Primula Dewi
AU - Ally Kafesa
AU - Mochammad Aqilah Herdiansyah
AU - Rr.Aulia Rahmawati Kusuma Putri
AU - Liew Kai Bin
AU - Intan Zarina Zainol Abidin
PY - 2026
DA - 2026/10/21
JO - Scientific Reports
DO - 10.1038/s41598-026-73503-w
UR - https://www.nature.com/articles/s41598-026-73503-w
AB - Tumor-associated macrophages (TAMs) frequently exhibit M2-like properties that support tumor progression. Deoxycholic acid (DCA), a secondary bile acid with amphiphilic membrane activity and context-dependent immunomodulatory effects, may influence macrophage phenotype. This study developed mannose-targeted DCA-loaded nanoliposomes and evaluated their physicochemical characteristics, cell-associated uptake, cytotoxicity, and effects on polarization-associated markers in THP-1-derived M2-like macrophages. Cellular uptake was assessed qualitatively by DiI fluorescence microscopy in two replicate experiments. Cytotoxicity was evaluated by MTT assay over 0.25-100 µM, and CD80/CD206 expression was assessed by flow cytometry after exposure to 10 or 20 µM DCA for 48 h. The targeted formulation had a mean hydrodynamic diameter of 155.1 ± 0.34 nm, a PDI of 0.28, a zeta potential of -12.8 ± 0.6 mV, spherical morphology, and an encapsulation efficiency of 82.94%. HPLC showed a DCA-associated peak at 6.215 min in the reference standard, disrupted DCA-loaded liposomes, and the unencapsulated fraction, whereas no corresponding peak was detected in the mobile-phase or blank-liposome controls. The formulation produced concentration-dependent cytotoxicity, with an estimated IC ₅₀ of 13.47 µM. At 20 µM for 48 h, the percentage of CD206-positive cells changed from 76.8 ± 2.31% to 21.7 ± 1.98%, whereas the percentage of CD80-positive cells changed from 18.6 ± 1.72% to 68.3 ± 2.54%. Because 20 µM exceeded the estimated IC ₅₀ , these observations may partly reflect selective cell loss. Flow-cytometric measurements were performed in triplicate (n = 3), but confirmation in independent biological experiments remains necessary. Additional viability-matched and functionally validated experiments are required.
SN - 2045-2322
ER -