Yan Chengyun, Chen Dawei, Gu Jiwei, Qin Jing
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, R. P. China.
J Pharm Pharmacol. 2006 Sep;58(9):1177-81. doi: 10.1211/jpp.58.9.0003.
N-Succinyl-chitosan has favourable properties as a drug carrier, such as biocompatibility, low toxicity and long-term retention in the body. It is a good candidate for cancer chemotherapy as a polymeric drug carrier. This study describes the preparation and characterization of 5-fluorouracil-loaded N-succinyl-chitosan nanoparticles (5-FU-Suc-Chi/NP) by an emulsification solvent diffusion method. The influence of the initial 5-FU concentration on the nanoparticle characteristics and release behaviour in phosphate-buffered saline solution (PBS) was evaluated. The Suc-Chi nanoparticles had a particle diameter (Z-average) in the range 202 approximately 273 nm and a negative zeta-potential (approx. -27 to -18 mV). The formulation with an initial 5-FU concentration of 1000 microg mL-1 provided the highest loading capacity (19%) and the highest extent of release (61% at 24 h). The 5-FU-Suc-Chi/NP showed good anti-tumour activity against Sarcoma 180 solid tumour and mild toxicity. According to the data obtained, this Suc-Chi-based nanotechnology opens new and interesting perspectives for cancer chemotherapy.
N-琥珀酰壳聚糖作为药物载体具有良好的性能，如生物相容性、低毒性和在体内的长期滞留性。作为一种聚合物药物载体，它是癌症化疗的良好候选者。本研究描述了通过乳化溶剂扩散法制备负载5-氟尿嘧啶的N-琥珀酰壳聚糖纳米粒（5-FU-Suc-Chi/NP）及其表征。评估了初始5-FU浓度对纳米粒特性以及在磷酸盐缓冲盐水溶液（PBS）中释放行为的影响。琥珀酰壳聚糖纳米粒的粒径（Z-平均）在202至273nm范围内，zeta电位为负（约-27至-18mV）。初始5-FU浓度为1000μg mL-1的制剂具有最高的载药量（19%）和最高的释放程度（24小时时为61%）。5-FU-Suc-Chi/NP对肉瘤180实体瘤显示出良好的抗肿瘤活性且毒性轻微。根据所获得的数据，这种基于琥珀酰壳聚糖的纳米技术为癌症化疗开辟了新的、有趣的前景。
