Paclitaxel-loaded stealth liposomes: Development, characterization, pharmacokinetics, and biodistribution

Figures & data

Figure 1. 3D structure of Paclitaxel.

Figure 2. Transmission electron microscope images of PTX-loaded stealth liposomes.

Figure 3. The PTX release profiles of free PTX (blue line), PTX-loaded stealth liposomes (dotted line), PTX-loaded stealth liposomes with rat plasma (1:1, v/v, red line) in PBS (pH 7.4) containing 0.1% Tween 80 (n = 3).

Figure 4. Mean plasma concentration-time profiles of PTX-loaded stealth liposomes (blue line), PTX injection (green line), and PTX conventional liposomes (red line). (Each group represents mean ± SD of six rats).

Table I. Pharmacokinetic parameters of 5 mg/kg PTX-loaded stealth liposomes, PTX injection and PTX conventional liposomes (n = 6).

Parameters	Injection	Conventional liposomes	Stealth liposomes
t1/2(h)	5.6 ± 1.4	13.7 ± 2.4	34.2 ± 4.5 *^#
Cmax(ng/mL)	3367.6 ± 362.5	3128.1 ± 326.3	4219.5 ± 437.5 ^#
AUC0-t (μg·h/mL)	121.4 ± 19.5	232.6 ± 24.1	410.7 ± 43.2 *^#
AUC0-∞ (μg·h/mL)	147.6 ± 21.4	267.3 ± 28.2	487.1 ± 51.6 *^#
MRT (h)	6.2 ± 2.1	15.7 ± 3.2	37.5 ± 4.2 *^#
CL (L/h)	14.8 ± 4.5	6.8 ± 2.3	4.8 ± 1.6 *

*P < 0.05: stealth liposomes versus injection.

^#P < 0.05: stealth liposomes versus conventional liposomes.

Figure 5. Tissue sections isolated on 48 h after treatment and stained with hematoxylin and eosin for histopathological evaluation. (A) Liver. (B) Spleen (× 200). (a) PTX injection. (b) PTX conventional liposomes and (c) PTX-loaded stealth liposomes.

Table II. AUC_0-t of different tissue of PTX injection, PTX conventional liposomes, and PTX-loaded stealth liposomes (n = 5).

	AUC0-t (μg·h/g) or (μg·h/mL)
Parameters	Tumor	Liver	Spleen	Plasma
Injection	98.6 ± 13.3	96.7 ± 11.7	76.4 ± 8.5	117.5 ± 14.2
Conventional liposomes	207.6 ± 39.6	302.6 ± 37.4	389.5 ± 43.2	228.8 ± 34.1
Stealth liposomes	378.6 ± 36.5*^#	178.2 ± 15.2*^#	235.5 ± 23.5*^#	410.8 ± 46.4*^#

*P < 0.05: stealth liposomes versus injection.

^#P < 0.05: stealth liposomes vs. conventional liposomes.