Aspartic acid derivatized hydroxylated fullerenes as drug delivery vehicles for docetaxel: an explorative study

Figures & data

Figure 1. Pictorial representation of synthetic scheme of C₆₀-OH-APA-DTX conjugate.

Figure 2. FT-IR spectrum of: (A) Fullerenols; (B) C₆₀-OH-APA and (C) C₆₀-OH-APA-DTX conjugate.

Figure 3. ¹H NMR spectrum of: (A) Fullerenol with deuterium exchange and (B) C₆₀-OH-APA-DTX conjugate.

Figure 4. X-ray diffraction patterns of: (A) Naïve fullerenes; (B) Fullerenols; (C) Pure DTX and (D) C₆₀-OH-APA-DTX conjugate.

Figure 5. FE-SEM images at X for: (A) naïve fullerenes and (B) C₆₀-OH-APA-DTX conjugate.

Table 1. Results of particle size, poly dispersity index (PDI) and zeta potential studies.

S. No	Name of sample	Particle size (nm)	PDI	Zeta potential (mV)
1	Naïve fullerenes	324.30 ± 1.24	0.49 ± 0.04	−2.71 ± 0.21
2	C60-OH	108.90 ± 1.03	0.37 ± 0.03	−2.78 ± 0.29
3	C60-OH-APA	68.06 ± 0.76	0.29 ± 0.05	−3.41 ± 0.41
4	C60-OH-APA-DTX	24.36 ± 0.65	0.17 ± 0.02	−7.99 ± 0.48

Figure 6. Graphs showing % drug release of pure DTX and C₆₀-OH-APA-DTX conjugate at pH 5.6 and 7.4 respectively at t = 24 h.

Figure 7. Bar graph showing % cell viability of pure DTX and C₆₀-OH-APA-DTX conjugate at various concentrations.

Figure 8. Confocal laser scanning microphotographs of (A) Control and (B) C₆₀-OH-APA-DTX treated group.

Table 2. Various pharmacokinetic parameters obtained from in-vivo pharmacokinetic studies.

S. No	Parameters	DTX	C60-OH-APA-DTX
1	[AUC]0–∞ (µg h ml^−1)	1025.62 ± 0.93	5986.71 ± 1.16*
2	t1/2 (h)	1.25 ± 0.04	7.84 ± 0.09*
3	K (h^−1)	0.10 ± 0.02	0.08 ± 0.005
4	Vd (l)	0.36 ± 0.01	1.16 ± 0.02*
5	Cl (l.h^−1)	1.53 ± 0.03	0.10 ± 0.02*

*Indicates the obtained data is significant.