269
Cyclodextrin ground nanosponges are widely used to augment
the solubility of the lipophilic drugs; the oral solubility of nifedipine was enhanced by incorporating into β-CD and diphenyl carbonate NS. The fabricated batch displayed enhanced oral
bioavailability (C max 0.02 μg/mL for test and 0.055 μg/mL for
control formulation), while the area under the moment curve
(AUMC) and AUC were 4.8 μg h
2
/mL and 0.056 μg h/mL,
respectively, with a mean residence time of 8.57 h. Stability studies
rendered nifedipine-laden NS stable in terms of particle size, drug
entrapment, and drug release. Hence, it can be concluded that
nifedipine-laden β-CD NS bids a potential drug delivery system for
oral delivery of the active molecule [88].
Gabapentin (GBP) is a BCS class III drug used as a primary drug
therapy for the treatment of partial seizures in pediatric as well as
geriatric patients. The bioavailability of GBP decreases with
increase in dose due to its absorption via saturable transport system and also due to other substrates following the same system.
The bitter taste is another problem associated with oral administration of this drug. A controlled-release formulation could
potentially minimize the saturation uptake transporter, in that
way that enhances absorption and avoids any potential side
effects. The dry powder suspension of GBP-loaded β-CD NSs
was used as a sustained- release carrier; desired controlled-release
profile for 12 h and insignificant drug leaching were observed in
reconstituted suspension during storage for 7 days at 45 C/75%
RH. NSs effectively masked the taste of gabapentin and released
retarding polymers as ethyl cellulose and Eudragit RS-100 pro2.11 Cyclodextrin
Nanosponges
for Anti-seizure
HO
HO
O
O
O
O
OH
H
H
H
H
H
H
OH
OH
OH
H 2 N
3
2
5
4
a
b
b
b
b b
c
c
c
c
6
1
7
d
d
d
d
e
e
e
e
F1
3.0
3.0
3.5
3.5
4.0
4.0
4.5
4.5
5.0
5.0
5.5
5.5
6.0
6.0
6.5
6.5
7.0
7.0
5.6
5.6
5.6
3
3 a
a
3
2
2
2
4
1
4
1
F2 (ρρη)
HO
O
HO
H5
OH
(b)
(a)
H3
H 2 N
a
b
c
d
e
(ρρη)
Fig. 6 (a) ROESY experiment results. (b) Schematic representation of β-CD interaction with L-DOPA [6]
Drug-Encapsulated Cyclodextrin Nanosponges
Cyclodextrin ground nanosponges are widely used to augment
the solubility of the lipophilic drugs; the oral solubility of nifedipine was enhanced by incorporating into β-CD and diphenyl carbonate NS. The fabricated batch displayed enhanced oral
bioavailability (C max 0.02 μg/mL for test and 0.055 μg/mL for
control formulation), while the area under the moment curve
(AUMC) and AUC were 4.8 μg h
2
/mL and 0.056 μg h/mL,
respectively, with a mean residence time of 8.57 h. Stability studies
rendered nifedipine-laden NS stable in terms of particle size, drug
entrapment, and drug release. Hence, it can be concluded that
nifedipine-laden β-CD NS bids a potential drug delivery system for
oral delivery of the active molecule [88].
Gabapentin (GBP) is a BCS class III drug used as a primary drug
therapy for the treatment of partial seizures in pediatric as well as
geriatric patients. The bioavailability of GBP decreases with
increase in dose due to its absorption via saturable transport system and also due to other substrates following the same system.
The bitter taste is another problem associated with oral administration of this drug. A controlled-release formulation could
potentially minimize the saturation uptake transporter, in that
way that enhances absorption and avoids any potential side
effects. The dry powder suspension of GBP-loaded β-CD NSs
was used as a sustained- release carrier; desired controlled-release
profile for 12 h and insignificant drug leaching were observed in
reconstituted suspension during storage for 7 days at 45 C/75%
RH. NSs effectively masked the taste of gabapentin and released
retarding polymers as ethyl cellulose and Eudragit RS-100 pro2.11 Cyclodextrin
Nanosponges
for Anti-seizure
HO
HO
O
O
O
O
OH
H
H
H
H
H
H
OH
OH
OH
H 2 N
3
2
5
4
a
b
b
b
b b
c
c
c
c
6
1
7
d
d
d
d
e
e
e
e
F1
3.0
3.0
3.5
3.5
4.0
4.0
4.5
4.5
5.0
5.0
5.5
5.5
6.0
6.0
6.5
6.5
7.0
7.0
5.6
5.6
5.6
3
3 a
a
3
2
2
2
4
1
4
1
F2 (ρρη)
HO
O
HO
H5
OH
(b)
(a)
H3
H 2 N
a
b
c
d
e
(ρρη)
Fig. 6 (a) ROESY experiment results. (b) Schematic representation of β-CD interaction with L-DOPA [6]
Drug-Encapsulated Cyclodextrin Nanosponges