Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting

Figures & data

Table 1. Composition of nanoemulsion formulations.

Formulation	Oil (Capmul MCM) (% w/w)	Surfactant Tween 80 (% w/w)	Co-surfactant PEG 400 (% w/w)	Water (% w/w)
F1	4	6	2	88
F2	4	11.2	3.8	81
F3	4	15.75	5.25	75
F4	6	6	2	86
F5	6	11.2	3.8	79
F6	6	15.75	5.25	73
F7	8	6	2	84
F8	8	11.2	3.8	77
F9	8	15.75	5.25	71

Figure 1. Microscopic images illustrate the histopathological condition of nasal mucosa after 2 h exposure of (A, negative control) PBS pH 6.4; (B, positive control) IPA; (C) drug-loaded nanoemulsion.

Figure 2. SQVM concentration–time profiles after intranasal administration of nanoemulsion and IV administration of PDS at 100 µg doses in rats brain (A) and blood (B).

Table 2. Pharmacokinetics parameters of SQVM following nasal and intravenous administration.

Formulation and route of administration	Organ/ Tissue	Cmax(ng)	Tmax (min)	T1/2 (min)	AUC0-180min (ng/ml*min)	AUC0-∞ (ng/ml*min)
Nanoemulsion (nasal)	Brain	24625.78 ± 644.40	60 ± 0.0	47.21 ± 0.98	2313384 ± 59962.05	2721980 ± 62740.91
Nanoemulsion (nasal)	Blood	17827.20 ± 2020.54	60 ± 0.0	47.27 ± 0.65	1687509 ± 186021.6	1993401 ± 215167.9
PDS (intra venous)	Brain	668.07 ± 151.09	50 ± 17.32	56.71 ± 37.84	54444.33 ± 10221.94	62167.65 ± 4686.593
PDS (intra venous)	Blood	6000.66 ± 343.26	15.05 ± 0.03	64.78 ± 14.87	1159375 ± 8324.267	458042.8 ± 15732.07

PDS, plain drug suspension.

Figure 3. Scintigraphy image of rat at (A) 0 h and (B) 1.0 h following intranasal administration of drug loaded nanoemulsion.