Yu Cui-Yun, Zhang Xi-Chen, Zhou Fang-Zhou, Zhang Xian-Zheng, Cheng Si-Xue, Zhuo Ren-Xi
Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, People's Republic of China.
Int J Pharm. 2008 Jun 5;357(1-2):15-21. doi: 10.1016/j.ijpharm.2008.01.030. Epub 2008 Jan 24.
Alginate based microparticle drug delivery systems were prepared for the sustained release of antineoplastic drugs. Two drugs, 5-fluorouracil (5-FU) and tegafur, were encapsulated into the microparticles. The drug loaded microparticles were fabricated using a very convenient method under very mild conditions, i.e., directly shredding the drug loaded beads into microparticles in a commercial food processor. The mean sizes of the obtained microparticles were between 100 and 200 microm. To effectively sustain the drug release, alginate microparticles were reinforced by chitosan during gelation. The drug release from the chitosan-reinforced alginate microparticles was obviously slower than that from the unreinforced microparticles. The effect of the reinforcement conditions on the drug release property of the microparticles was studied, and the optimized concentration of chitosan solution for reinforcement was identified. The effects of drug feeding concentration and pH value of the release medium on the drug release were investigated.
制备了基于藻酸盐的微粒药物递送系统用于抗肿瘤药物的缓释。将两种药物，5-氟尿嘧啶（5-FU）和替加氟，封装到微粒中。载药微粒采用非常简便的方法在非常温和的条件下制备，即在商用食品加工机中将载药珠子直接粉碎成微粒。所得微粒的平均尺寸在100至200微米之间。为了有效维持药物释放，在凝胶化过程中用壳聚糖增强藻酸盐微粒。壳聚糖增强的藻酸盐微粒的药物释放明显慢于未增强的微粒。研究了增强条件对微粒药物释放性能的影响，并确定了用于增强的壳聚糖溶液的最佳浓度。研究了药物进料浓度和释放介质pH值对药物释放的影响。
