Preparation of surface multiple-coated polylactide acid drug-loaded nanoparticles for intranasal delivery and evaluation on its brain-targeting efficiency

Figures & data

Figure 1. Scheme of preparing M-C-PLA-NPs coated with various kinds of materials.

Figure 2. Scanning electron micrographs of M-C-PLA-NP (10⁵ × magnification, A); Size distribution chart of M-C-PLA-NP (B) and Zeta potential distribution chart of M-C-PLA-NP (C).

Figure 3. Scanning electron micrograph of M-C-PLA-NP after lysozyme incubated for 2 h (10⁵ × magnification, A) and Size distribution chart of M-C-PLA-NP after lysozyme incubated for 2 h (B).

Figure 4. The curve of M-C-PLA-NP cumulative release percentage in pH 7.4 or pH 4.0 PBS. Data represented the mean ± SD.

Figure 5. Different tissues concentration-time profiles of aniracetam following nasal administration of M-C-PLA-NP (▪) and aniracetam solution (—) at a dose of M-C-PLA-NP of 50 µl (aniracetam content of 6.667 mg/ml). Data represented the mean ± SD.

Table 1. The results of targeting efficiency evaluation (n = 3).

	M-C-PLA-NP			Aniracetam solution
Tissues	AUC	Te	Cmax	AUC	Te	Cmax	Ce	Re
Brain	34.36 ± 0.99*	–	3.37 ± 0.15*	6.62 ± 0.81	–	1.05 ± 0.10	3.21 ± 0.33	5.19 ± 0.58
Heart	19.27 ± 0.72	1.783 ± 0.33	2.15 ± 0.08	8.36 ± 0.48	0.767 ± 0.11	1.42 ± 0.08	1.51 ± 0.05	2.31 ± 0.21
Spleen	5.49 ± 0.46	6.259 ± 0.18	0.54 ± 0.03	7.67 ± 0.23	0.863 ± 0.13	0.98 ± 0.02	0.55 ± 0.04	0.72 ± 0.07
Plasma	30.6 ± 0.65	1.123 ± 0.21	2.32 ± 0.37	7.90 ± 0.56	0.838 ± 0.05	1.20 ± 0.17	1.93 ± 0.30	3.87 ± 0.74
Lung	8.96 ± 0.19	3.835 ± 0.27	0.82 ± 0.06	5.41 ± 0.32	1.223 ± 0.10	0.40 ± 0.08	2.05 ± 0.08	1.66 ± 0.12
Liver	7.40 ± 0.82	4.643 ± 1.31	0.91 ± 0.33	33.50 ± 0.30	0.198 ± 0.02	2.16 ± 0.28	0.42 ± 0.19	0.22 ± 0.06
Kidney	16.72 ± 0.81	2.055 ± 0.34	2.44 ± 0.59	13.31 ± 0.42	0.497 ± 0.05	1.83 ± 0.25	1.33 ± 0.20	1.26 ± 0.12

Data represented the mean ± SD (n = 3).

AUC and C_max in M-C-PLA-NP group exhibited significant increase compared with that in control group, *p < 0.05.