Table 1
Ingredients list for preparation of FU microemulsion.
| Ingredient | Property |
|---|---|
| 5-FU | Drug |
| Tween 20 | Surfactant |
| Isopropyl alcohol | Cosurfactant |
| Isopropyl myristate | Oil |
| DMSO | Penetration enhancer |
| Rutin | Antioxidant |
Table 2
Solubility of R-5FU in different oils, surfactants and co-surfactants.
| Oil | Solubility(mg/ml) |
| Isopropyl myristate | 165.28 |
| Oleic acid | 183.12 |
| Castor oil | 44.26 |
| Olive oil | 32.61 |
| Surfactant | Solubility (mg/ml) |
| Tween 80 | 105.28 |
| Tween 20 | 93.12 |
| Span 80 | 58.27 |
| Span 20 | 31.62 |
| Cosurfactant | Solubility (mg/ml) |
| Isopropyl alcohol | 107.28 |
| Ethanol | 43.12 |
| N-butanol | 58.27 |
| Polyethylene glycol | 69.62 |
| Propylene glycol | 79.62 |
Figure 1
Phase diagram of 1:1 weight ratio of microemulsion.
Figure 2
Phase diagram of 2:1 weight ratio of microemulsion.
Figure 3
Phase diagram of 3:1 weight ratio of microemulsion.
Figure 4
Transmission electron microscopic surface area of prepared microemulsion batches.
Figure 5
Viscosity of microemulsion batches.
Figure 6
Graph of pH values of microemulsion batches.
Figure 7
Globules size range of prepared microemulsion batches.
Table 5
Values of drug permeation of prepared microemulsion batches.
| Time | 5-FU | RME1 | RME2 | RME3 |
|---|---|---|---|---|
| Absorption | Absorption | Absorption | Absorption | |
| 0 min | 0.128 | 0.128 | 0.135 | 0.138 |
| 1 min | 0.130 | 0.145 | 0.152 | 0.156 |
| 2 min | 0.161 | 0.165 | 0.174 | 0.178 |
| 3 min | 0.182 | 0.193 | 0.203 | 0.208 |
| 4 min | 0.217 | 0.232 | 0.244 | 0.251 |
| 5 min | 0.275 | 0.291 | 0.305 | 0.312 |
| 10 min | 0.358 | 0.386 | 0.406 | 0.416 |
| 30 min | 0.510 | 0.581 | 0.61 | 0.625 |
| 60 min | 1.012 | 1.161 | 1.22 | 1.25 |
| 3 hours | 1.012 | 1.161 | 1.22 | 1.25 |
Figure 8
Comparative skin retention profile for the all the formulation 5-FU
Figure 9
Percentage (%) mean cumulative 5-FU microemulsions penetration in skin.
Table 6
Scoring for irritation testing (HET-CAM assay).
| 0.5 min | 2 min | 5 min | ||||
|---|---|---|---|---|---|---|
| RME1 | Lysis | -- | -- | -- | 0 | Non-irritant |
| Hemorrhage | -- | -- | -- | |||
| Coagulation | -- | -- | -- | |||
| RME2 | Lysis | - | -- | -- | 0 | Non-irritant |
| Hemorrhage | -- | -- | -- | |||
| Coagulation | -- | -- | -- | |||
| RME3 | Lysis | -- | -- | -- | 0 | Non-irritant |
| Hemorrhage | -- | -- | -- | |||
| Coagulation | -- | -- | -- | |||
| Control (0.9%NaCl) | Lysis | -- | -- | -- | 0 | non-irritant |
| Hemorrhage | -- | -- | -- | |||
| Coagulation | -- | -- | -- | |||
| Irritant (0.1 N NaOH) | Lysis | -- | 7 | -- | 23 | Severe-irritant |
| Hemorrhage | 7 | -- | -- | |||
| Coagulation | 9 | -- | -- |
Table 7
Effects of RME1, RME2, RME3, control and irritant on chorioallantoic membrane with different time interval.
| Groups: - | |||
|---|---|---|---|
| RME1 |
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| RME2 |
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| RME3 |
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| Control |
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| Irritant |
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Figure 10
Acute skin irritation test of prepared microemulsion batches (a) RME 1, (b) RME 2, (c) RME 3 and control (d).