Anti-tumor effect of all-trans retinoic acid loaded polymeric micelles in solid tumor bearing mice.
OBJECTIVE
All-trans retinoic acid (ATRA) polymeric micelles were developed for parenteral administration. The distribution characteristics and antitumor activities of ATRA polymeric micelles were evaluated after intravenous administration to mice bearing CT26 solid tumors.


METHODS
ATRA incorporated in poly(ethylene glycol)-poly(benzyl aspartate) block copolymer was prepared by the evaporation method. The levels of [3H]ATRA in blood and tissue including tumor were determined by measuring the radioactivity after injection into mice. The tumor volume and the survival of the mice were determined to assess the anticancer activity.


RESULTS
The delivery of ATRA by polymeric micelles prolonged the blood circulation and enhanced the accumulation of ATRA in the tumor tissue compared with the administration of free ATRA. Tumor growth was significantly delayed and the survival time of mice was prolonged following the treatment by ATRA polymeric micelles demonstrating the improved anticancer activity of ATRA.


CONCLUSIONS
Polymeric micelles are a promising and effective carrier of ATRA in order to enhance tumor delivery and they have a promising potential application in the treatment of solid tumors.
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto, 606-8501, Japan.
Narin
N
Chansri
Shigeru
S
Kawakami
Masayuki
M
Yokoyama
Tatsuhiro
T
Yamamoto
Pensri
P
Charoensit
Mitsuru
M
Hashida
D000818:Animals; D008297:Male; D051379:Mice; D008823:Micelles; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000401:mortality; D014018:Tissue Distribution; D014212:Tretinoin / Q000008:administration & dosage* / Q000493:pharmacokinetics
D008823:Micelles; D014212:Tretinoin