TABLE 3.
Formulations of MG.
| Carrier | Proportion | Drug loading (%) | Entrapment efficiency (%) | Solubility (mg ml−1) | Bioavailability | References | ||
|---|---|---|---|---|---|---|---|---|
| Pluronic F127 and L61 (8:1; MG-M) | — | 27.58 ± 0.53 | 81.57 ± 1.49 | 3.62 ± 0.02 | The Cmax, AUC0-∞, Tmax, and T1/2 values of MG-M were 0.823 mg ml−1, 4.673 ± 0.31 mg/ml h, 0.75 ± 0.158 h, and 2.982 ± 0.528 h, respectively. The relative bioavailability of MG-M was 283% greater than that of raw MG. | Shen H et al. (2018) | ||
| SOL: HS15 40:10 | — | 4.12 ± 0.16 | 98.37 ± 1.23 | — | The Cmax, AUC0-∞, Tmax, and T1/2 values of MG-H were 0.837 ± 0.050 μg ml−1, 5.127 ± 0.988 μg/ml h, 0.708 ± 0.188 h, and 3.656 ± 1.212 h, respectively. The relative oral bioavailability of MG-H increased by 2.98-fold. | Ding et al. (2018) | ||
| SOL: TPGS 50: 6 | — | 4.03 ± 0.19 | 94.61 ± 0.91 | — | The Cmax, AUC0-∞, Tmax, and T1/2 values of MG-T were 0.918 ± 0.040 μg ml−1, 6.027 ± 0.963 mg/ml h, 0.750 ± 0.158 h, and 3.407 ± 0.855 h, respectively. The relative oral bioavailability of MG-T increased by 2.39-fold. | Ding et al. (2018) | ||
| Phospholipids, cholesterol, and mPEG2000-DSPE | Phospholipids: cholesterol: mPEG 2000-DSPE: MG 60:8:3:20 | — | 98.22 | — | Compared with MG solution, the liposome had a sustained-release effect. | Shen et al. (2016) | ||
| Soy lecithin | Soy lecithin: MG 0.27:0.8 | — | — | — | The cumulative dissolution rate was 96.3%, in 12 h. And the bioavailability was increased by 1.38 times, with the value of Cmax for 533.62 ± 59.01 ng ml−1. | Liu et al. (2020) | ||
| PVP K30 | PVPK30:MG 0.27:1.35 | — | — | — | The cumulative dissolution rate was 76.4%, in 12 h. And the bioavailability was increased by 2.12 times, with the value of Cmax for 721.73 ± 103.44 ng ml−1. | |||
| Povidone S-630 (PS-630) | PSS-630: MG 6:1 | — | — | — | The value of relative bioavailability, AUC0-t, T1/2, and Cmax was 137.22%, 823.81 ± 152.63 ng/L h, 6.066 ± 1.879 h, and 304.59 ± 136.48 ng L−1. | Li et al. (2019) | ||
| HPC | HPC: MG 6:1 | — | — | — | The values of bioavailability, AUC0-t, T1/2, and Cmax were 170.88%, 1025.90 ± 149.93 ng/L h, 17.63 ± 5.020 h, and 151.75 ± 26.37 ng L−1, respectively. | |||
| Eudragit EPO (EPO) | EPO: MG 6:1 | — | — | — | The values of bioavailability, AUC0-t, T1/2, and Cmax were 79.50%, 477.30 ± 159.46 ng/L h, 13.81 ± 11.780 h, and 83.49 ± 22.37 ng L−1, respectively. | Lin et al. (2014) | ||
| EPC and DPPC | 0.075 mg mL−1 MG | — | 74.13 ± 1.97 (EPC), 64.26 ± 2.92 | — | The EPC and DPPC liposomes enhanced the activity of inhibiting VSMC. | Chen (2008) | ||
| PVP | PVP: MG 1:1 | — | — | 105 | The Cmax, AUC0-∞, and Tmax, values of solid dispersion were 0.6 ± 0.1 nmol ml−1, 679.0 ± 130.0 nmol/ml−1 min, and 275.0 ± 272.6 min, respectively. | Lin et al. (2014) | ||
| CHC | MG concentration from 0.05 to 0.2 mg ml−1 | 79.3 ± 2.2 (0.2 mg ml−1), 88.4 ± 2.3 (0.2 mg ml−1), and 91.6 ± 0.4 (0.2 mg ml−1) | — | — | Compared with free MG, MG-CHC nanoparticles showed better cell uptake efficiency, antiproliferation, and inhibition of VSMC migration. | Wang et al. (2011) | ||
| Oil phase mass fraction of 20 wt% and an aqueous phase mass fraction of 80 wt% | The amount of MG was 2.0 g/100 ml | — | — | — | The absolute bioavailability of MG is 17.5 ± 9.7%. The AUC0-∞, T1/2, CL/F, and Vd/F values of MG emulsion (25 mg kg−1, i.v.) were 6,875 ± 1,080 μg/ml h, 5.49 ± 1.77 h, 2.9 ± 0.9 ml/h/kg, and 0.37 ± 0.059 ml/kg, respectively. The Cmax, AUC0-∞, Tmax, T1/2, CL/F, and Vd/F values of MG emulsion (50 mg kg−1, oral administration) were 426.4 ± 273.8 ng ml−1, 2665 ± 1,306 μg/ml h, 1.2 ± 1.6 h, 4.9 ± 3.0 h, 2.2 ± 1.0 ml/h/kg, and 13.9 ± 5.1 ml kg−1, respectively. | Sheng et al. (2014) | ||
| Distearoyl phosphatidylcholine (DSPC), DPPC, and dimyristoyl phosphatidylcholine (DMPC) | — | — | 84.87 ± 1.97 (DSPC), 75.05 ± 3.93 (DPPC), and 67.19 ± 2.92 (DMPC) | — | The three kinds of lipid could increase the inhibition activity of MG to VSMC, and the efficacy of inhibition was DMPC > DPPC > DSPC. | Chen (2009) | ||
| HP-β-CD | HP-β-CD: MG 10:1 | — | — | — | The water solubility of HP-β-CD-MG was more than 500 times higher than that of MG, and the stability of HP-β-CD-MG was significantly increased. | Qiu et al. (2016) | ||
| Uio-66(Zr) | — | — | 72.16 ± 2.15 | — | The Cmax, AUC0-∞, Tmax, and T1/2 values of MG@Uio-66(Zr) (100 mg kg−1, oral administration) were 3.77 ± 0.33 μg ml−1, 2099.95 ± 148.48 μg/ml min, 196.97 ± 17.38 min, and 206.21 ± 27.95 min, respectively. The Cmax, AUC0-∞, Tmax, and T1/2 values of MG@Uio-66(Zr) (100 mg kg−1, i.p.) were 5.65 ± 2.41 μg ml−1, 3831.72 ± 451.57 μg/ml min, 114.27 ± 7.09 min, and 606.35 ± 114.37 min, respectively. The relative bioavailability increased almost two-fold. | Santos et al. (2020) | ||
| Soluplus VR and Poloxamer 188 | MG: Soluplus VR: Poloxamer 188 1:12:5(MG-loaded mixed micelles (MMs)) and 2:1:1(MG nanosuspensions (MNs)) | 5.46 ± 0.65% (MMs) and 42.50 ± 1.57% (MNs) | 89.58 ± 2.54% (MMs) | — | The Cmax, AUC0-∞, Tmax, and T1/2 values of MMs were 0.587 ± 0.048 mg L−1, 2.904 ± 0.465 μg/L h, 0.792 ± 0.102 h, and 3.142 ± 0.285 h, respectively. The Cmax, AUC0-∞, Tmax, and T1/2 values of MNs were 0.65 ± 0.125 mg L−1, 2 2.217 ± 0.332 μg/L h, 0.5 h, and 2.776 ± 0.417 h, respectively. The gastrointestinal absorption of MG was increased by 2.85 and 2.27 times by MM and MN, respectively. | Li G et al. (2020) | ||
| PVP K-30 | MG: PVP K-30 1:1 | — | — | — | The Cmax, AUC0-∞, and Tmax values of solid dispersion were 0.6 ± 0.1 nmol ml−1, 679.0 ± 130.0 nmol/min mL, and 275.0 ± 272.6 min, respectively. | Lin et al. (2014) | ||