Página 1 de 8
Ti le:
Enginee ing Robus , Po ous Gua Gum Hyd ogels by One-S ep Mild
Syn hesis: Impac o Po ogen Choice on Rheology and Sus ained
Gas o e en i e Amoxicillin Deli e y [Da ase ].
Au ho s:
Fá ima Díaz-Ca asco; M.-Violan e de-Paz*; Ma ea Ka a ić; Es e anía Ga cía-Pulido; Ál a o
San os-Medina; Lucía Muíña-Ramil; M. G acia Ga cía-Ma ín; Elena Beni o.
* Co espondence: [email protected].
A ilia ion:
Depa amen o de Química O gánica y Fa macéu ica, Uni e sidad de Se illa, C/ P o . Ga cía
González, n.º 2, 41012-Se illa, España.
Resea che
email
ORCID
Fá ima Díaz-Ca asco
[email protected]
0009-0001-5922-0548
M.-Violan e de-Paz*
[email protected]
0000-0002-6544-4732
Ma ea Ka a ić
---
Es e anía Ga cía-Pulido
es ga [email protected]
Ál a o San os-Medina
al [email protected]
Lucía Muíña-Ramil
lucmui [email protected]
M.-G acia Ga cía-Ma ín
g [email protected]
0000-0002-7171-5236
Elena Beni o
ebeni [email protected]
0000-0002-8796-6873
Página 2 de 8
Con en
Ti le: .......................................................................................................................................... 1
Au ho s: ................................................................................................................................. 1
A ilia ion: .............................................................................................................................. 1
Keywo ds: .............................................................................................................................. 3
Abb e ia ions: ........................................................................................................................... 3
Da a o deg adabili y o GG-sys ems. ......................................................................................... 4
AMOX elease om single-s ep p epa ed and loaded o mula ions .............................................. 5
PEG used as po ogen ............................................................................................................. 5
(pH 2.0) .............................................................................................................................. 5
(pH 5.0) .............................................................................................................................. 5
Suc ose used as po ogen ....................................................................................................... 6
(pH 2.0) .............................................................................................................................. 6
(pH 5.0) .............................................................................................................................. 6
AMOX elease om pos -loaded IPN ........................................................................................... 7
PEG used as po ogen ............................................................................................................. 7
(pH 2.0) .............................................................................................................................. 7
(pH 5.0) .............................................................................................................................. 7
Suc ose used as po ogen ....................................................................................................... 8
(pH 2.0) .............................................................................................................................. 8
(pH 5.0) .............................................................................................................................. 8
Página 3 de 8
Keywo ds:
Gua gum hyd ogel; In e pene a ing polyme ne wo k ; (IPN); Diels-Alde c osslinking; one-po syn hesis;
po osi y modula ion; PEG po ogen; suc ose po ogen; Gas o e en i e d ug deli e y sys ems; GRDDS.
Abb e ia ions:
AMOX: amoxicillin; GG: gua gum; IPN: in e pene a ing polyme ne wo k; PEG: po osogen polye hylene
glycol-350; Suc: po osogen suc ose; ₅₀ (h): ime (h) o 50% deg ada ion o o mula ion mass.
Página 4 de 8
Da a o deg adabili y o GG-sys ems.
NAME and pH*
KEY
Deg adabili y o e ime (h): pe cen age o IPN mass emaining
₅₀ (h)**
1
2
3
4
5
6
7
8
24
48
F1 (pH 2.0)
GG-DA-AMOX25
82
72
66
61
56
46
38
33
11
0
5.02
F1 (pH 5.0)
GG-DA-AMOX25
85
77
71
66
61
52
44
39
17
0
6.16
F2 (pH 2.0)
GG-DA-AMOX40
79
67
60
54
49
39
31
26
7
0
3.94
F5 (pH 5.0)
GG-DA-AMOX40
83
73
66
60
55
45
37
32
14
0
5.02
F3 (pH 2.0)
GG-DA-PEG5-AMOX25
96
92
89
87
84
80
77
75
35
0
13.9
F3 (pH 5.0)
GG-DA-PEG5-AMOX25
97
93
91
88
86
82
80
78
42
0
15.5
F4 (pH 2.0)
GG-DA-PEG5-AMOX40
95
90
87
84
81
76
73
70
29
0
12.18
F4 (pH 5.0)
GG-DA-PEG5-AMOX40
96
92
89
86
83
79
76
73
36
0
13.65
F5 (pH 2.0)
GG-DA-PEG10-AMOX25
94
88
83
79
75
69
64
60
20
0
9.73
F5 (pH 5.0)
GG-DA-PEG10-AMOX25
95
90
85
81
77
72
68
64
27
0
8.93
F6 (pH 2.0)
GG-DA-PEG10-AMOX40
93
86
80
75
71
64
59
55
16
0
8.56
F6 (pH 5.0)
GG-DA-PEG10-AMOX40
94
88
83
78
74
68
64
60
23
0
9.81
F7 (pH 2.0)
GG-DA-PEG50-AMOX25
92
84
77
71
66
58
52
47
12
0
7.33
F7 (pH 5.0)
GG-DA-PEG50-AMOX25
93
86
80
75
71
64
59
55
19
0
8.71
F8 (pH 2.0)
GG-DA-PEG50-AMOX40
90
80
72
65
59
50
43
38
8
0
5.96
F8 (pH 5.0)
GG-DA-PEG50-AMOX40
92
83
76
70
65
57
51
46
15
0
7.25
F9 (pH 2.0)
GG-DA-Suc5-AMOX25
94
89
85
82
79
74
70
67
29
0
11.57
F9 (pH 5.0)
GG-DA-Suc5-AMOX25
95
91
87
84
81
77
73
70
35
0
12.85
F10 (pH 2.0)
GG-DA-Suc5-AMOX40
92
84
78
73
69
62
56
52
19
0
8.19
F10 (pH 5.0)
GG-DA-Suc5-AMOX40
93
86
81
76
72
66
61
57
25
0
9.37
F11 (pH 2.0)
GG-DA-Suc10-AMOX25
90
80
73
67
62
54
47
42
13
0
6.54
F11 (pH 5.0)
GG-DA-Suc10-AMOX25
92
83
76
71
66
59
53
48
20
0
9.37
F12 (pH 2.0)
GG-DA-Suc10-AMOX40
88
77
69
62
56
47
40
34
9
0
5.44
F12 (pH 5.0)
GG-DA-Suc10-AMOX40
90
80
72
66
60
52
45
40
16
0
6.37
F13 (pH 2.0)
GG-DA-Suc50-AMOX25
86
73
64
56
50
40
32
26
6
0
4.44
F13 (pH 5.0)
GG-DA-Suc50-AMOX25
88
77
69
62
56
47
40
34
13
0
5.52
F14 (pH 2.0)
GG-DA-Suc50-AMOX40
84
69
59
50
43
32
23
16
3
0
5.44
F14 (pH 5.0)
GG-DA-Suc50-AMOX40
87
74
64
56
49
39
31
25
10
0
4.47
* pH a which he deg ada ion s udy was conduc ed; ** Time (h) o 50% deg ada ion o o mula ion mass
Página 5 de 8
AMOX elease om single-s ep p epa ed and loaded o mula ions
PEG used as po ogen
(pH 2.0)
AMOX elease om single-s ep p epa ed and loaded o mula ion (PEG, pH 2.0)
PEG5-AMOX25
PEG5-AMOX40
PEG10-AMOX25
PEG10-AMOX40
PEG50-AMOX25
PEG50-AMOX40
Time (h)
F3
e o
F4
ERROR
F5
e o
F6
ERROR
7
ERROR
F8
ERROR
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1.00
44.27
2.39
60.88
3.04
20.79
2.27
55.72
2.79
17.34
0.15
13.49
0.70
2.00
54.21
1.94
80.97
1.62
27.78
0.08
67.89
1.36
22.17
2.60
16.75
0.41
3.00
78.83
13.32
85.95
4.30
29.95
1.69
70.06
3.50
22.24
1.14
17.62
0.50
5.00
71.59
0.47
94.44
0.94
31.00
0.75
77.19
0.77
23.62
0.07
18.91
0.71
8.00
82.41
1.45
100.00
2.00
36.56
1.95
78.59
1.57
26.48
1.67
19.63
0.71
(pH 5.0)
AMOX elease om single-s ep p epa ed and loaded o mula ion (PEG, pH 5.0)
PEG5-AMOX25
PEG5-AMOX40
PEG10-AMOX25
PEG10-AMOX40
PEG50-AMOX25
PEG50-AMOX40
Time (h)
F3
e o
F4
ERROR
F5
e o
F6
ERROR
7
ERROR
F8
ERROR
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1.00
42.82
8.11
60.54
3.03
19.30
1.61
27.46
1.37
32.17
4.65
12.00
2.09
2.00
51.36
3.72
77.20
3.09
22.44
0.66
38.34
1.53
18.46
0.75
13.31
0.32
3.00
57.99
2.21
78.73
3.94
25.88
0.15
47.37
2.37
19.78
0.67
15.28
0.43
5.00
94.57
3.95
88.24
2.65
27.88
0.15
55.57
1.67
21.31
0.51
16.75
0.31
8.00
78.64
6.98
89.99
4.50
30.60
0.10
62.54
3.13
24.12
0.95
18.64
0.35
Página 6 de 8
Suc ose used as po ogen
(pH 2.0)
AMOX elease om single-s ep p epa ed and loaded o mula ion (Suc, pH 2.0)
Suc5-AMOX25
Suc5-AMOX40
Suc10-AMOX25
Suc10-AMOX40
Suc50-AMOX25
Suc50-AMOX40
Time (h)
F9
e o
F10
ERROR
F11
e o
F12
ERROR
F13
ERROR
F14
ERROR
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1.00
26.19
0.76
14.39
0.50
20.84
0.51
17.17
0.08
15.96
2.05
9.63
4.35
2.00
34.66
0.91
17.94
0.88
16.59
0.38
20.64
1.19
17.37
0.31
11.77
3.05
3.00
40.90
1.58
20.26
0.71
18.46
1.32
35.12
4.57
20.55
0.25
13.83
2.26
5.00
74.96
1.54
36.46
0.84
22.02
0.93
28.20
2.52
22.80
0.17
14.67
1.99
8.00
65.55
1.04
37.28
4.05
25.27
0.09
27.60
2.77
24.76
0.51
17.00
2.12
(pH 5.0)
AMOX elease om single-s ep p epa ed and loaded o mula ion (Suc, pH 5.0)
Suc5-AMOX25
Suc5-AMOX40
Suc10-AMOX25
Suc10-AMOX40
Suc50-AMOX25
Suc50-AMOX40
Time (h)
F9
e o
F10
ERROR
F11
e o
F12
ERROR
F13
ERROR
F14
ERROR
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1.00
45.97
0.61
16.66
1.41
8.65
0.14
11.09
1.46
17.09
0.08
14.59
0.11
2.00
40.22
3.80
16.73
0.04
40.23
0.08
24.18
2.05
43.07
1.13
20.20
0.23
3.00
55.75
3.33
18.83
1.05
49.88
0.16
25.24
2.63
46.57
1.12
20.65
0.12
5.00
70.56
1.15
19.92
1.21
56.17
0.43
27.49
0.02
47.81
1.83
21.13
0.42
8.00
72.00
4.66
21.88
1.72
61.00
0.66
29.58
0.04
44.33
2.11
23.26
0.59
Página 7 de 8
AMOX elease om pos -loaded IPN
PEG used as po ogen
(pH 2.0)
AMOX elease om pos -loaded IPN (PEG, pH 2.0)
PEG5-AMOX25
PEG5-AMOX40
PEG10-AMOX25
PEG10-AMOX40
PEG50-AMOX25
PEG50-AMOX40
Time (h)
B3.4-AMOX25
e o
B3.4-AMOX40
ERROR
B5.6-AMOX25
e o
B5.6-AMOX40
ERROR
B7.8-AMOX25
ERROR
B7.8-AMOX40
ERROR
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1.00
32.70
3.23
48.84
2.10
17.72
7.66
1.64
0.12
9.30
8.02
8.39
7.25
2.00
50.61
9.66
57.11
5.98
44.33
3.59
39.11
8.67
41.73
1.48
44.40
14.91
3.00
61.34
0.28
52.70
3.45
57.56
0.33
55.65
1.73
54.87
4.73
57.76
6.86
5.00
69.99
1.63
60.05
1.98
81.43
0.59
60.29
2.03
65.72
0.32
61.92
0.29
8.00
72.49
0.41
61.54
0.82
91.06
2.33
63.73
0.34
75.68
5.81
63.99
0.89
(pH 5.0)
AMOX elease om pos -loaded IPN (PEG, pH 5.0)
PEG5-AMOX25
PEG5-AMOX40
PEG10-AMOX25
PEG10-AMOX40
PEG50-AMOX25
PEG50-AMOX40
Time (h)
B3.4-AMOX25
e o
B3.4-AMOX40
ERROR
B5.6-AMOX25
e o
B5.6-AMOX40
ERROR
B7.8-AMOX25
ERROR
B7.8-AMOX40
ERROR
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1.00
36.87
1.21
22.77
0.86
10.54
9.27
9.38
6.62
0.86
0.23
1.07
0.07
2.00
53.54
10.91
41.76
2.42
34.89
10.86
32.51
8.79
17.12
2.08
17.46
3.93
3.00
64.59
1.30
45.12
4.76
48.24
9.58
43.92
1.47
34.41
3.85
35.78
3.89
5.00
69.39
0.90
58.10
3.18
67.67
7.54
49.01
0.78
53.69
14.98
40.34
2.17
8.00
71.39
0.25
65.16
4.78
68.61
6.32
75.06
12.24
76.38
4.08
53.77
3.51
Página 8 de 8
Suc ose used as po ogen
(pH 2.0)
AMOX elease om pos -loaded IPN (Suc, pH 2.0)
Suc 5%
Suc 10%
Suc 50%
B9.10-AMOX25
B9.10-AMOX40
B11.12-AMOX25
B11.12-AMOX40
B13.14-AMOX25
B13.14-AMOX40
(h)
AMOX 25%
e o
40%
ERROR
25%
e o
40%
ERROR
25%
e o
40%
ERROR
0
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1
56.89
13.61
55.83
4.80
11.09
8.67
7.16
1.51
65.66
20.76
52.98
3.87
2
74.19
3.63
60.59
0.67
60.34
20.27
23.13
7.62
69.28
6.25
59.31
2.03
3
92.36
18.20
68.62
0.18
60.16
4.82
40.99
6.89
84.02
3.86
69.88
6.77
5
93.10
11.70
75.60
2.79
60.56
3.69
43.76
6.56
79.79
0.13
70.09
7.51
8
100.00
11.45
79.65
3.82
63.09
2.16
44.43
6.48
82.78
0.22
71.63
9.88
(pH 5.0)
AMOX elease om pos -loaded IPN (Suc, pH 5.0)
Suc 5%
Suc 10%
Suc 50%
B9.10-AMOX25
B9.10-AMOX40
B11.12-AMOX25
B11.12-AMOX40
B13.14-AMOX25
B13.14-AMOX40
(h)
AMOX 25%
e o
40%
ERROR
25%
e o
40%
ERROR
25%
e o
40%
ERROR
0
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
0.00
1
59.43
15.26
51.46
5.45
11.90
1.23
14.24
2.25
55.43
20.61
7.25
0.33
2
78.96
1.14
61.12
6.69
32.25
2.27
31.19
8.62
70.63
7.32
53.73
3.21
3
86.62
2.79
67.64
7.18
56.32
10.26
39.69
10.51
78.75
3.05
63.98
4.73
5
96.00
2.19
72.10
5.97
61.82
5.74
42.97
10.46
83.61
0.49
71.23
6.04
8
100.1
9.57
72.29
2.86
62.00
6.73
44.22
8.63
83.36
0.30
70.57
2.39