Biocompatible poly(methylidene malonate)-made materials for pharmaceutical and biomedical applications

Breton, Pascal; Larras, Virginie; Roy, Didier; Sagodira, Serge; Limal, David; Bonnafous, David; Colin, Nathalie; Bru, N.; Fattal, Elias; Couvreur, Patrick

doi:10.1016/j.ejpb.2007.08.003

Cited by 4 publications

(1 citation statement)

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“…7 -10 A biodegradable polymer is a promising candidate for drug-delivery applications. 8,[11][12][13] We studied the in vitro degradation, drug release, in vivo degradation, and tissue biocompatibility of 5-FU-PGSs for a series of PGS implants loaded with 5-FU (5-FU-PGSs). 4 Although PGS is a potential biodegradable drug carrier, 4 there are two major problems with sustained release of 5-FU-PGSs: (1) 5-FU is loaded but not conjugated in the PGS, which limits the doped amount; (2) the cumulative drug release profiles of 5-FU-PGSs exhibit a biphasic release with an initial burst release in the first day and 100% cumulative release of 5-FU after 7 days, which means that the release rate is very fast.…”

Section: Introductionmentioning

confidence: 99%

A poly(glycerol-sebacate-(5-fluorouracil-1-acetic acid)) polymer with potential use for cancer therapy

Sun

et al. 2012

Journal of Bioactive and Compatible Polymers

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In this study, 5-fluorouracil-1-acetic acid was chemically conjugated with poly(glycerol-sebacate) (PGS) to form a unitary polymer poly(glycerol-sebacate- (5-fluorouracil-1-acetic acid)) (PGS-5-FU-CH2COOH). The structure, the in vitro antitumor activity of 5-FU-CH2COOH, the in vitro degradation, the drug release, and antitumor activity as well as the in vivo degradation and tissue biocompatibility of PGS-5-FU-CH2COOH were investigated. The 5-FU-CH2COOH inhibited HeLa (human cervical cancer cell line) and SGC-7901 (human gastric adenocarcinoma cell line) tumor cells with a half maximal inhibitory concentration (IC50) of 0.196 and 0.267 μM, respectively, after a 3-day incubation. The in vitro drug release profiles of PGS-5-FU-CH2COOH exhibited a biphasic release with an initial exponential phase in the first week and then the second constant linear phase. An in vitro antitumor assay of the PGS-5-FU-CH2COOH polymer showed significant cytotoxicity against tumor cells. The implanted PGS-5-FU-CH2COOH degraded completely in 1 month after implantation. The antitumor activity and improved drug release profile of PGS-5-FU-CH2COOH indicate its potential as an implantable polymer for cancer therapy.

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