Table 3.
Comparison between various solidification process of su-SEDDS.
Process | Physical State of Pre-Concentrate [213] | Solvent Use 1 | Description/Advantages (A) and Disadvantages (D) [30,131,212] | Max Loading Capacity (%, w/w) 2 [30,213] | Suitable Drug Dose/Potency [30] | Self-Emulsification Rate [30] | Ref. | ||
---|---|---|---|---|---|---|---|---|---|
O | X | Drug | Lipid Vehicle | ||||||
Physical adsorption | L 3 | √ | Adsorption onto solid carrier using physical blending with a mixer -A: Easy and Low cost, Easy scale-up -D: Low adsorption efficiency (large amount of solid carrier) and exudation of liquid lipid by tablet compaction |
10 | 80 | Low dose, high potency | ++ | [68,108,119] | |
Granulation/pelletization followed by drying | L 3, SS 4, S 5 | √ | Similar with conventional wet granulation -A: Easy and low cost, Excellent powder property, Flexible applicable to various solid dosage forms (including controlled release system), Easy scale-up -D: Destabilization by high temperature for drying |
- | - | Low dose, high potency | ++ | [5,127,211] | |
Spray drying | L 4, SS 4, S 5 | √ | Evaporation of solvent from atomized SEDDS with solid carrier -A: Narrow particle size distribution, Relatively easy scale-up -D: Destabilization or loss of drug and/or volatile component by high temperature for drying |
50 | 60 | Low dose, high potency | +++ | [113,114,115,215,220] | |
Freeze drying or Spray freeze-drying | L 3, SS 4, S 5 | √ | Lyophilization of solvent (mainly aqueous) from frozen SEDDS with solid carrier -A: Prevent destabilization or loss of drug and/or volatile by heat -D: Destabilization of drug by freezing and lyophilization, Low process efficiency, particle aggregation and poor re-dispersibility |
50 | 60 | Low dose, high potency | +++ | [221,222,223] | |
Spray congealing | SS 4, S 5 | √ | Spraying of molten formula with or without solid carrier into a cooling chamber -A: Prevent destabilization or loss of drug and/or volatile by heat, Solvent free -D: Destabilization of drug by freezing, Bad flow property, Limitations on the use of liquid lipids, particle aggregation and poor re-dispersibility |
30 | 99 | Low-medium dose | ++ | [224,225] | |
Melt granulation or Melt extrusion and spheronization | SS 4, S 5 | √ | High shear mixing at high temperature -A: High process efficiency, Solvent free -D: Destabilization or loss of drug and/or volatile component by high temperature for drying |
60–80 | 50 | Low-medium dose | ++ | [226,227] | |
Supercritical fluid (SCF) | L 3, SS 4, S 5 | √ | √ | Adsorption and/or coating onto solid carrier using high diffusivity of SCF -A: Mild condition, High loading efficiency -D: High cost for development of commercial scale equipment |
20 | 99 | Low-medium dose | +++ | [204,228,229] |
1 Whether the solvent is used or not, 2 The percentage of the mass ratio of a drug or vehicle that can be maximally loaded in the formulation, 3 Liquid, 4 Semi-solid, 5 Solid.