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Merck

Injectable intratumoral hydrogel as 5-fluorouracil drug depot.

Biomaterials (2013-01-25)
Hyo Won Seo, Da Yeon Kim, Doo Yeon Kwon, Jin Seon Kwon, Ling Mei Jin, Bong Lee, Jae Ho Kim, Byoung Hyun Min, Moon Suk Kim
ABSTRACT

The effectiveness of systemically administered anticancer treatments is limited by difficulties in achieving therapeutic doses within tumors, a problem that is complicated by dose-limiting side effects to normal tissue. To increase the efficacy and reduce the toxicity of systemically administered anticancer 5-fluorouracil (5-Fu) treatments in patients, intratumoral administration of an injectable hydrogel has been evaluated in the current work. The MPEG-b-(PCL-ran-PLLA) diblock copolymer (MCL) containing 5-Fu existed in an emulsion-sol state at room temperature and rapidly gelled in vivo at the body temperature. MCL acted as in vivo biodegradable drug depot over a defined experimental period. A single injection of 5-Fu-loaded MCL solution resulted in significant suppression of tumor growth, compared with repeated injection of free 5-Fu as well as saline and MCL alone. For both repeated injections of free 5-Fu and single injection of 5-Fu-loaded MCL, most of the 5-Fu was found in the tumor, indicating the maintenance of therapeutic concentrations of 5-Fu within the target tumor tissue and the prevention of systemic toxicity associated with 5-Fu in healthy normal tissues. In conclusion, this work demonstrated that intratumoral injection of 5-Fu-loaded MCL may induce significant suppression of tumor growth through effective accumulation of 5-Fu in the tumor.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Poly(ethylene glycol) methyl ether, average Mn 5,000
Sigma-Aldrich
Poly(ethylene glycol) methyl ether, average Mn 550
Sigma-Aldrich
Poly(ethylene glycol) methyl ether, BioUltra, 500
Sigma-Aldrich
Poly(ethylene glycol) methyl ether, average Mn ~2,000
Sigma-Aldrich
Poly(ethylene glycol) methyl ether, average Mn 750
Sigma-Aldrich
Poly(ethylene glycol) methyl ether, average Mn 10,000
Sigma-Aldrich
Poly(ethylene glycol) methyl ether, average Mn 20,000
Sigma-Aldrich
Methoxypolyethylene glycol 350, average mol wt 350