Table 1.
Composition |
In vitro measurements
c
|
||||||
Formula
a
|
Span® 60 (mg) |
Tween® 80 (mg) |
PE
b
|
EE% |
PS (nm) |
PDI |
ZP (mV) |
(a) | |||||||
F1 | 400 | 100 | – | 95.4 ± 1.7 | 240.9 ± 10.3 | 0.39 ± 0.03 | −32.1 ± 1.7 |
F1L | 400 | 100 | Labrasol® | 60.3 ± 3.0 | 439.5 ± 43.8 | 0.51 ± 0.12 | −37.9 ± 1.0 |
F1T | 400 | 100 | Transcutol® | 61.1 ± 3.9 | 563.6 ± 35.1 | 0.49 ± 0.17 | −37.9 ± 2.1 |
F1G | 400 | 100 | Tetraglycol® | 93.7 ± 2.2 | 471.3 ± 69.8 | 0.57 ± 0.18 | −38.6 ± 0.8 |
F2 | 300 | 200 | – | 75.3 ± 9.9 | 189.3 ± 3.3 | 0.57 ± 0.10 | −30.6 ± 1.5 |
F2L | 300 | 200 | Labrasol® | 50.5 ± 3.5 | 195.7 ± 4.0 | 0.53 ± 0.07 | −37.2 ± 1.0 |
F2T | 300 | 200 | Transcutol® | 47.5 ± 1.1 | 299.6 ± 8.3 | 0.76 ± 0.08 | −36.8 ± 1.2 |
F2G | 300 | 200 | Tetraglycol® | 72.5 ± 2.5 | 363.2 ± 20.7 | 0.57 ± 0.01 | −30.6 ± 2.2 |
(Q) (μg/cm2)
c
|
(J) (µg/cm2/h)
c
|
||||||
Formula
a
|
Q24 |
Q36 |
Q48 |
J24 |
J36 |
J48 |
|
(b) | |||||||
F1 | 32.2 ± 9.6 | 78.2 ± 7.8 | 184.5 ± 42.7 | 1.5 ± 0.5 | 2.2 ± 0.4 | 3.6 ± 0.8 | |
F1L | 93.1 ± 14.8 | 148.1 ± 3.56 | 208.8 ± 4.5 | 4.4 ± 0.7 | 4.5 ± 0.0 | 4.6 ± 0.00 | |
F1T | 73.9 ± 6.9 | 120.5 ± 11.8 | 201.3 ± 13.3 | 3.5 ± 0.3 | 3.6 ± 0.3 | 4.2 ± 0.1 | |
F1G | 56.1 ± 13.9 | 107.3 ± 17.4 | 204.5 ± 20.8 | 3.5 ± 1.2 | 3.6 ± 0.6 | 4.2 ± 0.0 | |
F2 | 60.6 ± 13.6 | 102.9 ± 9.0 | 158.1 ± 11.6 | 2.8 ± 0.6 | 3.1 ± 0.2 | 3.5 ± 0.2 | |
F2L | 86.3 ± 0.3 | 110.9 ± 23.2 | 236.4 ± 100.4 | 3.9 ± 0.1 | 3.4 ± 0.4 | 4.7 ± 1.6 | |
F2T | 72.6 ± 13.5 | 93.7 ± 20.8 | 209.8 ± 90.2 | 3.4 ± 0.6 | 3.0 ± 0.6 | 4.2 ± 1.6 | |
F2G | 59.1 ± 0.7 | 86.1 ± 1.6 | 147.7 ± 3.0 | 2.8 ± 0.0 | 2.7 ± 0.0 | 3.1 ± 0.1 | |
Hal solution | 2.7 ± 2.4 | 6.1 ± 0.5 | 16.6 ± 6.3 | 0.1 ± 0.1 | 0.2 ± 0.0 | 0.3 ± 0.0 |
PECSs: Penetration enhancer-containing spanlastics; PE: penetration enhancer; EE%: percentage entrapment efficiency; PS: particle size; PDI: polydispersity index; ZP: zeta potential.
All formulae contained 2.5 mg Hal/ ml and total volume was 10 ml.
PE concentration was 1 % w/v.
All values are reported as mean ± SD (n = 3).