Skip to main content
. Author manuscript; available in PMC: 2014 Jul 10.
Published in final edited form as: J Control Release. 2013 Apr 6;169(0):17–27. doi: 10.1016/j.jconrel.2013.03.033

Fig. 3. In vitro and in vivo antitumor activity of 4-(N)-GemC18-SLNs and 3′-(O)-GemC18-SLNs against TC-1 or TC-1-GR tumors.

Fig. 3

(A) The viability of TC-1 cells after incubation with various concentrations of gemcitabine HCl, 3′-(O)-GemC18-SLNs, or 4-(N)-GemC18-SLNs for 48 h (n = 4). aP < 0.001, 3′-(O)-GemC18-SLNs or 4-(N)-GemC18-SLNs vs. gemcitabine HCl; bP < 0.05, cP < 0.001, 4-(N)-GemC18-SLNs vs. 3′-(O)-GemC18-SLNs. (B) Viability of TC-1-GR cells after incubation with various concentrations of gemcitabine HCl, 3′-(O)-GemC18-SLNs, or 4-(N)-GemC18-SLNs for 48 h (n = 4). dP < 0.001, 4-(N)-GemC18-SLNs vs. gemcitabine HCl; eP < 0.05, 4-(N)-GemC18-SLNs vs. 3′-(O)-GemC18-SLNs. (C) The hydrolysis of gemcitabine from 3′-(O)-GemC18-SLNs or 4-(N)-GemC18-SLNs when incubated in RPMI 1640 medium at 37°C (n = 4). fP < 0.001, 3′-(O)-GemC18-SLNs vs. 4-(N)-GemC18-SLNs. (D) The levels of 3′-(O)-GemC18 or 4-(N)-GemC18 detected in TC-1-GR cells after incubation with 40 μM of 3′-(O)-GemC18-SLNs or 4-(N)-GemC18-SLNs at 37°C for up to 6 h (n = 3). (E) In vivo antitumor activity of 3′-(O)-GemC18-SLNs and 4-(N)-GemC18-SLNs against TC-1 tumors in Nu/Nu mice (n = 4–5). gP < 0.05 hP < 0.01 iP < 0.001 vs. mannitol control. (F) In vivo antitumor activity of 3′-(O)-GemC18-SLNs and 4-(N)-GemC18-SLNs against TC-1-GR tumors in Nu/Nu mice (n = 4–5). jP < 0.05, kP < 0.01, 4-(N)-GemC18-SLNs vs. mannitol; lP < 0.05, 4-(N)-GemC18-SLNs vs. 3′-(O)-GemC18-SLNs. (G) Levels of 3′-(O)-GemC18 or 4-(N)-GemC18 in TC-1-GR tumor tissues 6 h after i.v. injection of either 3′-(O)-GemC18-SLNs or 4-(N)-GemC18-SLNs (n = 3–4). mP < 0.01. (H) Plasma concentrations of 3′-(O)-GemC18 or 4-(N)-GemC18 in TC-1-GR tumor-bearing mice 6 h after i.v. injection of either 3′-(O)-GemC18-SLNs or 4-(N)-GemC18-SLNs (n = 3–4). nP < 0.05. (I) Representative Western blot of RRM1 protein in TC-1-GR tumor tissues 19 days after tumor cell injection. Mice were i.v. injected with 4-(N)-GemC18-SLNs or 3′-(O)-GemC18-SLNs 6 and 13 days after tumor cell injection. The dose of the GemC18 was 1 mg per injection per mouse (n = 3).

HHS Vulnerability Disclosure