• Asian Pacific Journal of Cancer Prevention
• /
• 제15권1호
• /
• pp.407-411
• /
• 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.

• 대한화학회지
• /
• 제57권1호
• /
• pp.88-93
• /
• 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.

• 폴리머
• /
• 제31권5호
• /
• pp.447-453
• /
• 2007

본 연구에서는 재결정 PLGA 분말을 진공 건조 방법을 사용하여 제조하였다. 5-FU가 함유된 PLGA 웨이퍼를 이용한 조절된 방출을 위하여 재결정 PLGA 분말의 응용성을 연구하기 위하여 세 종류의 웨이퍼를 제조하였다; 1) 순수한 PLGA, 2) 재결정 PLGA, 및 3) 순수한PLGA와 재결정 PLGA의 혼합(4 : 1, 1 : 1 및 1 : 4). 순수한 PLGA와 재결정 PLGA 분말은 NMR, IR과 GPC를 이용하여 비교 분석하였다. 주사전자현미경을 이용하여 제조한 웨이퍼 의 표면과 단면의 형태학적 차이를 관찰하였다. 웨이퍼로부터 방출된 5-FU의 방출거동은 HPLC를 이용하여 측정하였다. 5-FU/재결정 PLGA 웨이퍼는 5-FU/순수한 PLGA 웨이퍼에 비교하여 낮은 초기 방출과 지속적 방출거동을 갖는 것을 확인하였다. 순수한 PLGA/재결정 PLGA의 비율은 조절된 방출거동을 갖게 할 수 있음을 볼 수 있었다.