Synthesis, characterization of novel injectable drug carriers and the antitumor efficacy in mice bearing Sarcoma-180 tumor


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Abstract

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 C12-15 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 °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.

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