A nanoparticulate drug-delivery system for glaucocalyxin A: formulation, characterization, increased in vitro, and vivo antitumor activity

Figures & data

Figure 1. The chemical structure of glaucocalyxin A.

Figure 2. Characterization of GLA nanoparticles. (A) Particle size distribution of GLA nanosuspensions (n = 3); (B) TEM micrograph of GLA nanosuspensions ( × 50 000); (C) DSC thermograms for the freeze-dried GLA nanosuspensions, coarse drug powders, lecithin, and lyophilized powders of fetal calf serum (top to bottom).

Figure 3. Solubility profiles of the GLA coarse suspensions, GLA nanosuspensions, and GLA solution (n = 3).

Figure 4. The cytotoxicity of free GLA solution and GLA nanosuspensions on HepG2 cell lines after a 12-h exposure. The results are expressed as the mean ± SD (n = 6). *p < 0.05 (nanosuspensions versus solution).

Figure 5. (A) Tumor growth in H22 tumor-bearing mice at 10.0 mg/kg of GLA (n = 6). (B) Relative body weight changes in mice after i.v. administration. The results are expressed as the mean ± SD (n = 6).

Table 1. The in vivo antitumor effects of different formulations of GLA on H22 tumor-bearing mice.

Group	Dose (mg/kg)	Tumor weight (g)	Inhibition rate (%)	Spleen coefficient (10^−3)
Saline	–	1.95 ± 0.11	N. A.	7.94 ± 0.43
HCPT injection	10	0.42 ± 0.04**	78.46	7.36 ± 0.41
GLA nanosuspensions	10	0.89 ± 0.04**#	54.11	7.11 ± 0.42
GLA solution	10	1.25 ± 0.18**	36.02	7.57 ± 0.60

**p < 0.01 versus the normal saline group. #p < 0.05 versus the GLA solution group. Each value represents the mean ± SD (n = 6).