School of Pharmaceutical Sciences, Jilin University, Changchun, People's Republic of China.
Int J Nanomedicine. 2013;8:1499-506. doi: 10.2147/IJN.S41462. Epub 2013 Apr 18.
Surgical tumor resection is the main treatment for tumors however the treatment process often results in massive bleeding and tumor cell residue. The main aim of this research was to address problems such as bleeding, systemic chemotherapy side effects while enhancing quality of life, and increasing drug concentrations at the tumor site by developing a novel formulation with local long-term efficacy for treatment of tumors and to stop bleeding.
5-Fluorouracil (5-FU) was suspended in an ethyl acetate solution of poly D,L-lactide-co-glycolic acid (PLGA) and a vacuum drying method was applied. The hemostatic gelatin sponge loaded with 5-FU was prepared by absorption of the suspension. The in vitro and in vivo characteristics of the hemostatic gelatin sponge loaded with 5-FU (5-FU-HAGS) were investigated.
5-FU-HAGS (hemostatic absorbable gelatin sponge loaded with 5-fluorouracil) was successfully produced with controlled release of the content and was reproducibly suitable for local tumor treatment as an implant to stop bleeding. The encapsulation efficiency of 5-FU-HAGS was above 98%. The in vitro 5-FU release kinetic profile matched a near zero-order equation for 20 days. The in vivo 5-FU plasma concentration was at a more stable level than when 5-FU solution was administered by subcutaneous injection. Bleeding can be stopped more effectively by coating a piece of blank gelatin sponge. The survival ratio of tumor-bearing mice using a 5-FU-HAGS subcutaneous implant was higher when compared to mice given a subcutaneous injection of 5-FU solution.
The 5-FU-HAGS system is a potential and effective way of enhancing the survival ratio and improving the quality of life of tumor-bearing mice.
手术肿瘤切除是治疗肿瘤的主要方法,但治疗过程常导致大量出血和肿瘤细胞残留。本研究旨在通过开发一种新的局部长期疗效的治疗肿瘤和止血的制剂,解决出血、全身化疗副作用等问题,提高生活质量,增加肿瘤部位的药物浓度。
将 5-氟尿嘧啶(5-FU)悬浮在聚(D,L-乳酸-共-乙醇酸)(PLGA)的乙酸乙酯溶液中,并采用真空干燥法。通过吸收悬浮液制备载有 5-FU 的止血明胶海绵。研究了载有 5-FU 的止血明胶海绵(5-FU-HAGS)的体外和体内特性。
成功制备了 5-FU-HAGS(载有 5-氟尿嘧啶的止血可吸收明胶海绵),其内容物具有可控释放,可重复适用于局部肿瘤治疗作为止血植入物。5-FU-HAGS 的包封效率高于 98%。体外 5-FU 释放动力学曲线符合 20 天的近零阶方程。与皮下注射 5-FU 溶液相比,体内 5-FU 血浆浓度更稳定。用空白明胶海绵涂层可以更有效地止血。与皮下注射 5-FU 溶液的荷瘤小鼠相比,使用 5-FU-HAGS 皮下植入物的荷瘤小鼠的存活率更高。
5-FU-HAGS 系统是提高荷瘤小鼠存活率和改善生活质量的一种有潜力和有效的方法。