Effect of the structure of ginsenosides on the in vivo fate of their liposomes

Figures

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  Fig. 1. (A) The core structure of ginsenosides. (B) Ginsenoside structure with 0, 1, 2 glycosyl groups attached to position C-3, C-6 and C-20, respectively.

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  Fig. 2. Characteristics of liposomes. (A) Morphology of cholesterol liposomes and various ginsenoside liposomes (scale bar = 100 nm). (B) Size and PDI changes of cholesterol liposomes and various ginsenoside liposomes at 4 °C for 7 d.

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  Fig. 3. Micropolarity of liposomes. (A) The fluorspar spectra of pyrene. (B) Pyrene micro-polarity I1/I3 (378/383) in pure phospholipid liposomes (EPC), Chol-lipo and GS-lipos. (n = 3, mean ± SD). *P < 0.05, **P < 0.01,***P < 0.001.

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  Fig. 4. Pharmacokinetic profiles of various liposomes in ICR mice. The fluorescence intensity-time curves of ginsenoside liposomes with different numbers of glycosyl groups attached to positions C-3 (A), C-6 (B) and C-20 (C). (D-F) Pharmacokinetic parameters of ginsenoside liposomes with different glycosyl positions and quantities. (n = 3, mean ± SD). *P < 0.05, **P < 0.01, ***P < 0.001.

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  Fig. 5. The uptake of ginsenoside liposomes with different glycosyl positions and numbers by 4T1 tumor cells. (n = 3, mean ± SD). *P < 0.05, **P < 0.01, ****P < 0.0001.

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  Fig. 6. Tumor targeting of ginsenoside liposomes in vivo. (A) In vivo imaging of DiR-labeled in 4T1 tumor bearing mice. (B) In vivo imaging of tumors of Chol-lipo and GS-lipos. (C) Mean fluorescence intensity of tumor of Chol-lipo and GS-lipos. (D) Fluorescence images of biodistribution of Chol-lipo and GS-lipos in 4T1 tumor bearing mice 24 h. (n = 3; mean ± SD). **P < 0.01, ***P < 0.001.

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  Fig. 7. Molecular docking of ginsenosides with Glut 1. (A) Dock scores of cholesterol molecule and various ginsenosides docking with Glut 1. (B) 3D overlay interaction of Glut 1with cholesterol and ginsenosides. (n = 3, mean ± SD). *P < 0.05, ***P < 0.001.

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  Fig. 8. (A-C) The cellular uptake of ginsenoside liposomes with different number of glycosyl groups at C-3, C-6, C-20 positions by pre-saturated glucose receptor of 4T1 tumor cells (n = 3; mean ± SD), **P <0.01 and ***P <0.001. (D-F) The cellular uptake of ginsenoside liposomes with different number of glycosyl groups at C-3, C-6, C-20 ginsenoside liposomes before and after Glut 1 silencing. (n = 3; mean ± SD), **P <0.01 and ***P <0.001.