Electrosteric stealth Rivastigmine loaded liposomes for brain targeting: preparation, characterization, ex vivo, bio-distribution and in vivo pharmacokinetic studies

Figures & data

Figure 1. (A) Photomicrographs (40×) of ESS liposomes; (B) transmission-electron micrograph (TEM) of ESS liposomes.

Figure 2. (a) In vitro release profile of RHT from ESS liposomes in comparison with RHT solution. (b) In vitro release profile of RHT from ESS liposomes; fresh, after storage for one, and three months.

Figure 3. Permeation profile of Rivastigmine through sheep nasal mucosa in six hours from RHT solution, and ESS liposomes.

Figure 4. (a) Mean plasma concentration time curve; (b) mean brain concentration time curve of RHT in plasma after administration of groups 1 and 2.

Table 1. Mean pharmacokinetic parameters of Rivastigmine (rabbits plasma and brain) after receiving groups 1 and 2 intranasally.

	Mean ± SD
Parameters	Group 1Plasma	Group 2Plasma	Group 1Brain	Group 2Brain
Cmax (ng/ml)^a or (ng/g)^b	676.4 ± 242.2	581.6 ± 378.6	531.3 ± 309.4	875.1 ± 191.0
Tmax (h)	0.5 ± 0.0	2.7 ± 1.2	0.7 ± 0.3	4.0 ± 0.0
AUC0–t (ng/ml.h)^a or (ng/g.h)^b	551.5 ± 124.1	2336.7 ± 1350.3	892.3 ± 417.3	4243.9 ± 1507.2
AUC0–∞ (ng/ml.h)^a or (ng/g.h)^b	551.8 ± 123.0	2340.5 ± 1352.9	786.5 ± 300.6	4337.0 ± 1471.8
K (h^−1)	0.6 ± 0.2	0.6 ± 0.0
t1/2 (h)	1.3 ± 0.5	1.1 ± 0.0
MRT (h)	1.1 ± 0.1	3.5 ± 0.3	4.3 ± 2.1	5.0 ± 0.6
% Relative bioavailability		424.2		486

^aUnits of plasma data.

^b Units of brain data.