Table 2 |.
Summary of relative bioavailability and relative bioactivity values for proteins delivered with or without silica nanoparticle absorption enhancers in mice. Data is presented as arithmetic average ± standard error.
Bioactivity | ||||||
---|---|---|---|---|---|---|
Drug | Delivery Route | Dose | Silica NPs | rBGmin | AAC | rBA |
U/kg | % | % | ||||
Insulin (Healthy) | SQ | 1 | No | 50.1 ± 5.5 | 37.3 ± 13.6 | 100.0 ± 42.3 |
INT | 1 | No | 100.0 ± 0.0 | 0.0 ± 5.6 | 0.0 ± 0.0 | |
1 | Yes | 64.6 ± 7.5 | 37.3 ± 7.5 | 100.0 ± 33.1 | ||
Oral | 675 | No | 81.6 ± 3.9 | 0.0 ± 0.1 | 0.0 ± 0.0 | |
10 | Yes | 70.3 ± 4.3 | 13.2 ± 2.2 | 35.4 ± 11.1 | ||
40 | Yes | 60.3 ± 1.8 | 4.9 ± 0.7 | 13.3 ± 4.2 | ||
675 | Yes | 40.4 ± 7.2 | 0.5 ± 0.1 | 1.4 ± 0.4 | ||
Insulin (Hyper-glycaemic) | SQ | 1 | No | 38.4 ± 5.7 | 88.2 ± 17.1 | 100.0 ± 26.6 |
Oral | 10 | No | 103.1 ± 5.0 | 17.9 ± 11.0 | 0.0 ± 0.0 | |
10 | Yes | 75.5 ± 4.7 | 217.3 ± 48.6 | 29.1 ± 8.5 | ||
Insulin (Diabetic) | SQ | 1 | No | 25.2 ± 8.1 | 98.5 ±44.2 | 100.0 ± 2.4 |
Oral | 10 | No | 90.1 ± 6.2 | 376.7 ± 34.2 | 0.0 ± 0.0 | |
10 | Yes | 63.0 ± 10.7 | 376.7 ± 34.2 | 23.4 ± 4.9 | ||
Bioavailability | ||||||
Drug | Delivery Route | Dose | Silica NPs | Cmax | AUC | F |
U/kg | μU/ml | h * μU/ml | % | |||
Insulin (Healthy) | SQ | 1 | No | 52.5 ± 21.6 | 16.0 ± 5.2 | 100.0 ± 46.3 |
INT | 1 | Yes | 8.7 ± 1.9 | 13.6 ± 2.4 | 84.8 ± 31.5 | |
1 | No | 0.7 ± 0.6 | 0.5 ± 0.1 | 2.9 ± 1.2 | ||
U/kg | ng/ml | h * ng/ml | % | |||
Exenatide (Healthy) | SQ | 1 | No | 15.3 ± 1.4 | 20.2 ± 2.0 | 100.0 ± 13.7 |
Oral | 1 | Yes | 0.5 ± 0.2 | 2.0 ± 0.5 | 10.0 ± 2.3 | |
1 | No | 0.0 ± 0.0 | 0.3 ± 0.1 | 1.4 ± 0.4 |
rBGmin = minimum average relative blood sugar achieved. AAC = insulin dose adjusted area above the blood glucose curve. rBA = dose-adjusted relative bioactivity. Cmax = maximum average serum drug concentration achieved. AUC = dose adjusted area beneath the serum concentration curve. F = relative bioavailability.