Table 1
Independent variables with their levels and codes in BBD
| Independent variables (factors) | Levels | ||
|---|---|---|---|
| Low (−1) | Medium (0) | High (+1) | |
| X= PVA (%w/v) | 1.5 | 2 | 2.5 |
| Y= Stirring speed (rpm) | 750 | 875 | 1000 |
| Z= Stirring time (min) | 30 | 45 | 60 |
Table 2
BBD of the study and their observed responses
| Run | PVA (%w/v) | Stirring speed (rpm) | Stirring time (minutes) | PS (nm) | PDI | EE% |
|---|---|---|---|---|---|---|
| 1. | 0 | 0 | 0 | 2500 | 0.732 | 70.56 |
| 2. | +1 | 0 | −1 | 3950 | 0.283 | 82.64 |
| 3. | −1 | +1 | 0 | 1500 | 0.991 | 67.87 |
| 4. | 0 | +1 | −1 | 2820 | 0.785 | 53.57 |
| 5. | −1 | 0 | +1 | 4670 | 0.962 | 65.47 |
| 6. | +1 | 0 | +1 | 3800 | 0.214 | 89.18 |
| 7. | −1 | 0 | −1 | 3250 | 0.699 | 68.49 |
| 8. | +1 | −1 | 0 | 1600 | 0.308 | 98.36 |
| 9. | 0 | 0 | 0 | 2300 | 0.652 | 78.08 |
| 10. | 0 | −1 | +1 | 2950 | 0.685 | 73.61 |
| 11. | 0 | 0 | 0 | 2880 | 0.816 | 81.59 |
| 12. | −1 | −1 | 0 | 1540 | 0.708 | 71.38 |
| 13. | 0 | +1 | +1 | 4770 | 0.795 | 58.32 |
| 14. | +1 | +1 | 0 | 2500 | 0.211 | 64.32 |
| 15. | 0 | −1 | −1 | 3230 | 0.610 | 80.85 |
| 16. | 0 | 0 | 0 | 1980 | 0.592 | 69.14 |
| 17. | 0 | 0 | 0 | 2010 | 0.759 | 73.75 |
Figure 1
Calibration graph and absorption spectra at various concentrations of posaconazole
Figure 2
FTIR spectra of posaconazole (A), graphene (B), PVA (C), and PCZ-G (D)
Figure 3
FE-SEM image of PCZ-G
Figure 4
DSC thermogram of PCZ-G
Table 3
Physicochemical properties of optimized PCZ-G gel
| S.N. | Parameters | Observations |
|---|---|---|
| 1 | Color | Black |
| 2 | Odor | None |
| 3 | Consistency | Homogenous and smooth |
| 4 | Grittiness | Nil |
| 4 | pH | 5.89±0.03 |
| 5 | Viscosity | 15.377±6.37 Pa.s |
| 5 | Spreadability | 6.9±0.36 cm |
| 7 | Extrudability | 19.44±0.73 g/cm2 |
Table 4
Coded coefficient and p-value for that coefficient between experimental factors or its combinations and responses
| Constant | A | B | C | AXB | BXC | AXA | BXB | CXC | ||
|---|---|---|---|---|---|---|---|---|---|---|
| PS | Coefficient | 2334 | 111.25 | 283.75 | 367.5 | 117.95 | 557.5 | −37 | −512 | 1620.5 |
| p-value | 0.3841 | 0.049 | 0.018 | 0.3812 | 0.013 | 0.8291 | 0.017 | <0.0001 | ||
| PdI | Coefficient | 0.7102 | −0.293 | 0.058 | 0.034 | −0.095 | 0.016 | −0.167 | −0.011 | −0.003 |
| p-value | <0.0001 | 0.048 | 0.200 | 0.029 | 0.655 | 0.0017 | 0.739 | −0.927 | ||
| % EE | Coefficient | 74.62 | 7.661 | −10.01 | 0.128 | 0.00 | 2.99 | 5.35 | −4.49 | −3.53 |
| p-value | 0.0019 | 0.0004 | 0.937 | 0.00 | 0.224 | 0.044 | 0.079 | 0.150 |
Figure 5
Effect of independent variables on PS: (a) contour plots and (b) 3D response surface plots
Figure 6
Effect of independent variables on PDI: (a) contour plots and (b) 3D response surface plots
Figure 7
Effect of independent variables on EE%: (a) contour plots and (b) 3D response surface plots
Table 5
Parameters for optimization of posaconazole and graphene-loaded microparticle by BBD
| S. No. | Response | Goal |
|---|---|---|
| 1. | Average particle size (nm) | Minimize |
| 2. | PdI | Minimize |
| 3. | % EE | Maximize |
Table 6
Optimized solution by BBD
| Independent variables (factors) | Formulation parameter setting |
|---|---|
| A = PVA (%w/v) | 2.5 |
| B = Stirring speed (rpm) | 752.85 |
| C = Stirring time (min) | 52 |
Table 7
Validation of the experimental model
| S.No. | Dependent variables | Predicted value | Experimental value |
|---|---|---|---|
| 1. | R1= Average PS (nm) | 1499.98±338.915 | 1600±252.47 |
| 2. | R2= PDI | 0.280±0.069 | 0.308±0.029 |
| 3. | R3= %EE | 99.62±4.49 | 98.36±3.89 |
Table 8
In Vitro Drug Release Kinetics Model
| S. No. | In vitro drug release kinetics model | Parameters (R2 values) |
|---|---|---|
| 1. | Zero-order kinetics | 0.9638 |
| 2. | First-order kinetics | 0.6112 |
| 3. | Higuchi release kinetics | 0.9797 |
| 4. | Korsmeyer–Peppas model | 0.9619 |
Figure 8
In vitro drug release analysis
Figure 9
Antifungal activity of PCZ-G gel (A), plate showing zone of inhibition (B)