• Title/Summary/Keyword: Sustained-release 5-Fu

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Experimental Study on Sustained-release 5-Fluorouracil Implantation in Canine Peritoneum and Para-aortic Abdominalis

  • Wei, Guo;Nie, Ming-Ming;Shen, Xiao-Jun;Xue, Xu-Chao;Ma, Li-Ye;Du, Cheng-Hui;Wang, Shi-Liang;Bi, Jian-Wei
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.1
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    • pp.407-411
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    • 2014
  • Objective: To observe local and systemic toxicity after sustained-release 5-fluorouracil (5-Fu) implantation in canine peritoneum and para-aortic abdominalis and the changes of drug concentration in the local implanted tissue with time. Methods: 300 mg sustained-release 5-Fu was implanted into canine peritoneum and para-aorta abdominalis. Samples were taken 3, 5, 7 and 10 days after implantation for assessment of changes and systemic reactions. High performance liquid chromatography was applied to detect the drug concentrations of peritoneal tissue at different distances from the implanted site, lymphatic tissue of para-aortic abdominalis, peripheral blood and portal venous blood. Results: 10 days after implantation, the drug concentrations in the peritoneum, lymphatic tissue and portal vein remained relatively high within 5 cm of the implanted site. There appeared inflammatory reaction in the local implanted tissue, but no visible pathological changes such as cell degeneration and necrosis, and systemic reaction like anorexia, nausea, vomiting and fever. Conclusions: Sustained-release 5-Fu implantation in canine peritoneum and para-aortic abdominalis can maintain a relatively high tumour-inhibiting concentration for a longer time in the local implanted area and portal vein, and has mild local and systemic reactions. Besides, it is safe and effective to prevent or treat recurrence of gastrointestinal tumours and liver metastasis.

Preparation and In Vitro Release of Ramose Chitosan-Based-5-Fluorouracil Microspheres

  • Li, He-Ping;Li, Hui;Wang, Zhou-Dong;Zhang, Juan-Juan;Deng, Man-Feng;Chen, San-Long
    • Journal of the Korean Chemical Society
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    • v.57 no.1
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    • pp.88-93
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    • 2013
  • In order to construct a controlled release system of drugs and to reduce toxic side effects of 5-fluorouracil, the novel ramose chitosan-based-5-fluorouracil microspheres (CS-FU-MS) were prepared. Firstly, using chitosan (CS) as carriers and 5-fluorouracil (5-FU) as a model drug, ramose chitosan-based-5-fluorouracil (CS-FU) was efciently synthesized by chemical crosslinking method through microwave irradiation, drug loading was 10.6%; Secondly, CS-FU-MS were prepared by CS-FU self-assembled under the dialysis conditions and the free 5-FU was encapsulated further at the same time. The size dispersivity of particles is uniform, and the average diameter of the CS-FU-MS was $4{\mu}m$. The drug encapsulation efficiency was 76.1%, and the drug loading was increased to 26.22%. CS-FU-MS maintain the zero-order release time in PBS (pH = 7.4) and HCl/KCl (pH = 1.2) dialysis medium was 40h and 34h respectively, and the cumulative release were 58.89% and 79.33% in 182 h. The results showed that CS-FU-MS have excellent sustained release properties.

Effect of Recrystallized PLGA on Release Behavior of 5-Fluorouracil (재결정화된 PLGA의 특성에 따른 5-FU 웨이퍼의 방출거동)

  • Park, Jung-Soo;Lee, Joon-Hee;Choi, Myung-Gyu;Rhee, John-M.;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.31 no.5
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    • pp.447-453
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    • 2007
  • In this study, we fabricated recrystallized PLGA (rPLGA) particles using the vacuum drying method. In order to investigate an applicability of the rPLGA particles for controlled release system of 5-fluorouracil (5-FU) loaded PLGA wafer, we prepared three different wafers using; 1) untreated PLGA (uPLGA), 2) rPLGA, and 3) uPLGA and rPLGA (4 : 1, 1 : 1 or 1 : 4). The rPLGA particles were characterized using NMR, IR and GPC to compare with uPLGA particles. The surface and cross section morphology of the prepared wafers were observed by the scanning electron microscope. The release profile of the 5-FU loaded wafer was measured by HPLC. The 5-FU/rPLGA wafer released the incorporated 5-FU in a sustained manner with low initial burst compared to 5-FU/uPLGA. These results showed that the ratio of pure PLGA/recrystallized PLGA can affect the release behaviors.