Preparation of R848-loaded hydrophobic mesoporous silica nanoparticles and study on its effects on the repolarization of macrophages

doi:10.3877/cma.j.issn.2095-1221.2025.06.003

Abstract

Abstract:

Objective

Phenyl-modified mesoporous silica nanoparticles (PMSN) -loaded immunomodulator Resiquimod (R848) was prepared to investigate whether PMSN-R848 could repolarize M2-type macrophages to M1-type.

Methods

Mesoporous silica (MSN) was prepared by calcination, Phenyltriethoxysilane (PhTES) was added to modify MSN with phenyl and loaded with R848 to obtain PMSN-R848 nanoparticles. The drug loading efficiency of R848 on PMSN was calculated by measuring the R848 standard curve using an enzyme-linked immunosorbent assay (ELISA) reader. The structure of PMSN and PMSN-R848 was observed by transmission electron microscopy. The cytotoxicity of PMSN-R848 was assessed via the CCK-8 assay. Fluorescence electron microscopy (FEM) was employed to detect the colocalization of PMSN-R848 with macrophage lysosomes. Flow cytometry was performed to determine whether PMSN-R848 could repolarize macrophages. One-way analysis of variance was used for comparison between multiple groups, and LSD-t test was used for pairwise comparison between groups.

Results

The drug loading rate of PMSN loaded with R848 was (36.97 ± 5.80) %, the PMSN transmission electron microscope showed a spherical structure with pores, adsorbed particles could be seen on the surface of the spherical structure of PMSN-R848, PMSN-R848 was non-cytotoxic and could be well localized in macrophage lysosomes, and M2 macrophages were repolarized to the M1 phenotype after co-incubation with PMSN-R848.

Conclusion

The PMSN loaded with R848 could effectively repolarize M2 macrophages to M1.

Key words: Mesoporous silica, Macrophages, Resiquimod, Immunomodulation

Ting Zhang, Yanmei Zhang, Jiao Fan, Yu Pu, Li Zhang. Preparation of R848-loaded hydrophobic mesoporous silica nanoparticles and study on its effects on the repolarization of macrophages[J]. Chinese Journal of Cell and Stem Cell(Electronic Edition), 2025, 15(06): 339-345.

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URL: https://zhxbygxbzz.cma-cmc.com.cn/EN/10.3877/cma.j.issn.2095-1221.2025.06.003

https://zhxbygxbzz.cma-cmc.com.cn/EN/Y2025/V15/I06/339

Figures/Tables 7

References 24

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分组	CD86表达的百分比（%）	CD206表达的百分比（%）
IL-4	29.66 ± 0.20	49.30 ± 0.47
IL-4+PMSN	38.18 ± 2.55^a	51.47 ± 2.93
IL-4+R848	45.00 ± 2.25^ab	23.44 ± 2.40^ab
IL-4+PMSN-R848	46.92 ± 1.15^ab	22.09 ± 1.32^ab
LPS	52.67 ± 3.34^abc	8.91 ± 1.40^abcd
F值	48.740	283.900
P值	< 0.0 001	< 0.0 001

分组	CD86表达的百分比（%）	CD206表达的百分比（%）
IL-4	29.66 ± 0.20	49.30 ± 0.47
IL-4+PMSN	38.18 ± 2.55^a	51.47 ± 2.93
IL-4+R848	45.00 ± 2.25^ab	23.44 ± 2.40^ab
IL-4+PMSN-R848	46.92 ± 1.15^ab	22.09 ± 1.32^ab
LPS	52.67 ± 3.34^abc	8.91 ± 1.40^abcd
F值	48.740	283.900
P值	< 0.0 001	< 0.0 001

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