Enhanced brain targeting of temozolomide in polysorbate-80 coated polybutylcyanoacrylate nanoparticles

Figures & data

Figure 1 Chemical structure of TMZ.

Figure 2 TEM image of TMZ-PBCA-NPs prepared by emulsion polymerization. Bars represent 200 nm A) and 100 nm B).

Figure 3 FTIR spectra of TMZ, PBCA-NPs and TMZ-PBCA-NPs.

Figure 4 In vitro release profile of TMZ solution, TMZ-PBCA-NPs and TMZ-PBCA-NPs + polysorbate-80.

Table 1 The different release model of TMZ-PBCA nanoparticles (I) and TMZ-PBCA nanoparticles + polysorbate-80 II (n = 3)

Formulation	Model
	First order	Hixson-Crowell	Higuchi	Ritger- Peppas
	r	r	r	r	n
I	0.865	0.843	0.945	0.967	0.383
II	0.868	0.845	0.947	0.966	0.382

Table 2 Equations of standard curve of the organs and body distribution (in μg drug per g tissue, μg/g) after intravenous administration of different temozolomide formulations in rats (n=6)

Organ	Equation of standard curve	Formulation
		I	II	III
Heart	Y = 2.10 × 10^5X + 1.51 × 10^4 (r = 0.9974)	3.29 ± 0.23	2.19 ± 0.29	1.68 ± 0.26
Liver	Y = 1.86 × 10^5X + 1.32 × 10^4 (r = 0.9963)	3.26 ± 0.35	4.41 ± 0.46b	4.84 ± 0.47b
Spleen	Y = 2.03 × 10^5X + 2.39 × 10^4 (r = 0.9937)	2.11 ± 0.17	3.22 ± 0.31b	3.08 ± 0.25b
Lungs	Y = 2.09 × 10^5X + 2.01 × 10^4 (r = 0.9969)	1.95 ± 0.12a	2.47 ± 0.24b	2.20 ± 0.32a,b
Kidneys	Y = 1.85 × 10^5X + 2.63 × 10^4 (r = 0.9922)	5.17 ± 0.47	4.09 ± 0.37b	3.71 ± 0.30b
Brain	Y = 2.00 × 10^5X + 1.97 × 10^4 (r = 0.9972)	0.48 ± 0.11	0.71 ± 0.12	1.10 ± 0.19

Notes: I = TMZ solution; II = TMZ-PBCA nanoparticles; I = TMZ-PBCA nanoparticles + polysorbate-80. Level of significance according to the Tukey test P < 0.05. This level is reached between the different groups unless indicated by superscript letters:

a Nonsignificant difference between I and III;

b Nonsignificant difference between II and III.

Figure 5 In vivo different tissue distribution of temozolomide concentrations (μg/g) after intravenous injection of TMZ solution, TMZ-PBCA-NPs and TMZ-PBCA-NPs + polysorbate-80.