Y. Tokudome et al., ANTITUMOR-ACTIVITY OF VINCRISTINE ENCAPSULATED IN GLUCURONIDE-MODIFIED LONG-CIRCULATING LIPOSOMES IN MICE BEARING METH-A SARCOMA, Biochimica et biophysica acta. Biomembranes, 1279(1), 1996, pp. 70-74
Liposomes modified with the uronic acid derivative palmityl-D-glucuron
ide (PGlcUA) have a long-circulation time and tend to accumulate in th
e tumors of tumor-bearing mice. Taking advantage of this character, we
investigated the therapeutic effect of vincristine (VCR) encapsulated
in liposomes containing PGlcUA (dipalmitoylphosphatidylcholine/choles
terol/PGlcUA = 4:4:1 as a molar ratio) on tumor-bearing mice. VCR was
loaded into liposomes by a remote loading method, and then free or lip
osomal VCR was injected intravenously into BALB/c mice bearing Meth A
sarcoma implanted subcutaneously 5 days before hand. Single-dose admin
istration of VCR (3.0 mg/kg) in PGlcUA-liposomes significantly suppres
sed tumor growth, and prolonged the survival time (T/C = 1.37). Furthe
rmore, two-dose administration of the liposomes cured one third of the
animals. The therapeutic effect of PGlcUA-liposomes was greater than
that of control liposomes containing dipalmitoylphosphatidylglycerol i
nstead of PGlcUA. PGlcUA-liposomes might thus be a useful tool for del
ivering antitumor agents to tumor tissues.