Formulation and Optimization of Polymeric Nanoparticles for Intranasal Delivery of Lorazepam Using Box-Behnken Design: In Vitro and In Vivo Evaluation
Table 3
Distribution of 99mTc-lorazepam from LS (i.v.), LS (i.n.), and Lzp-PLGA-NPs (i.n.) at different time intervals in Sprague-Dawley rats*.
Formulation and route of administration
Distribution of lorazepam in blood and brain compartments at different Distribution sampling time points
Organ/tissue
0.5 h
1 h
2 h
4 h
8 h
LS (i.v)
Blood
2.976 ± 0.1
2.737 ± 0.15
2.350 ± 0.3
1.813 ± 0.25
1.524 ± 0.15
Brain
1.547 ± 0.2
1.512 ± 0.3
1.396 ± 0.32
0.826 ± 0.11
0.610 ± 0.12
LS (i.n)
Blood
1.404 ± 0.2
1.545 ± 0.2
1.210 ± 0.04
0.556 ± 0.16
0.359 ± 0.1
Brain
0.673 ± 0.2
1.148 ± 0.25
0.923 ± 0.2
0.335 ± 0.08
0.247 ± 0.2
Lzp-PLGA-NPs (i.n)
Blood
1.769 ± 0.3
1.916 ± 0.18
2.062 ± 0.18
2.125 ± 0.35
1.507 ± 0.1
Brain
1.399 ± 0.1
1.624 ± 0.23
1.794 ± 0.15
1.388 ± 0.22
0.104 ± 0.2
LS (i.v)
Brain/blood
0.519 ± 0.23
0.553 ± 0.25
0.594 ± 0.2
0.456 ± 0.05
0.400 ± 0.2
LS (i.n)
Brain/blood
0.479 ± 0.15
0.743 ± 0.1
0.763 ± 0.15
0.602 ± 0.1
0.687 ± 0.3
Lzp-PLGA-NPs (i.n)
Brain/blood
0.791 ± 0.2
0.847 ± 0.15
0.870 ± 0.1
0.653 ± 0.25
0.694 ± 2.5
The rats were administered 100 Ci 99mTc-lorazepam and the radioactivity was measured in percent per gram of tissue of the administered dose. Each value is the mean ± SD of three estimations. Radioactivity was measured at 0 h and all the measurements were performed using 0 h sample corresponding tissue/organ as blank sample.
