New unsaturated
polyesters of poly(
fumaric acid-glycol-
dodecanedioic acid) P(
FA-GLY-DDDA) copolymers, poly(
fumaric acid-glycol-
brassylic acid) P(
FA-GLY-BA) copolymers, poly(
fumaric acid-glycol-tetradecanedioic
acid) P(
FA-GLY-TA) copolymers and poly(
fumaric acid-glycol-pentadecanedioic
acid) P(
FA-GLY-PA) copolymers were prepared by melt polycondensation of the corresponding mixed monomers:
fumaric acid, glycol and one of C(12-15) dibasic
acids. The copolymers were characterized by FT-IR, gel permeation chromatography (GPC), and the surface structure of unsaturated
polyesters after solidify were studied by atomic force microscopy (AFM). The molecular structure and composition of the unsaturated
polyesters were determined by 1H NMR spectroscopy. In vitro studies showed that some of the copolymers are degradable in
phosphate buffer at 37 degrees C and have properly drug release rate as
drug carriers. The biocompatibility of P(
FA-GLY-DDDA) and P(
FA-GLY-BA) copolymers under mice skin was also evaluated, macroscopic observation and microscopic analysis demonstrated that the copolymer is biocompatible and well tolerated in vivo. Antitumor efficacy of P(
FA-GLY-DDDA) copolymers and P(
FA-GLY-BA) copolymers containing 5%
adriamycin hydrochloride (ADM) in mice bearing Sarcoma-180
tumor exhibited increased volume doubling time (VDT) (22+/-1.5 days and 24+/-2.5 days) compared to plain
subcutaneous injection of ADM (7+/-0.9 days). The antitumor efficacy of injecting P(
FA-GLY-DDDA)-ADM inside
tumor twice intervened in 22 days exhibited an especially increased cytotoxic effect as revealed by increased VDT (33+/-2.5 days), and the antitumor efficacy of injecting P(
FA-GLY-BA)-ADM inside
tumor twice intervened in 24 days exhibited an especially increased cytotoxic effect as revealed by increased VDT (35+/-1.5 days). The studies suggested that P(
FA-GLY-DDDA) copolymers and P(
FA-GLY-BA) copolymers as effective and
injectable carriers for
antineoplastic drug like
adriamycin hydrochloride have a very good foreground in the treatment of noumenon
tumor.