Nanoparticles of 5-fluorouracil (5-FU) loaded N-succinyl-chitosan (Suc-Chi) for cancer chemotherapy: preparation, characterization--in-vitro drug release and anti-tumour activity.
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.
Yan
Chengyun
C
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, R. P. China.
Chen
Dawei
D
Gu
Jiwei
J
Qin
Jing
J
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000737:chemistry* / Q000627:therapeutic use; D048271:Chitosan / Q000737:chemistry*; D003102:Colloids; D003692:Delayed-Action Preparations; D004058:Diffusion; D004337:Drug Carriers; D004339:Drug Compounding; D005472:Fluorouracil / Q000737:chemistry* / Q000627:therapeutic use; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles; D009368:Neoplasm Transplantation; D010316:Particle Size; D012510:Sarcoma 180 / Q000188:drug therapy / Q000473:pathology; D012995:Solubility; D013997:Time Factors
D000964:Antimetabolites, Antineoplastic; D003102:Colloids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; C118639:N-succinyl-chitosan; D048271:Chitosan; D005472:Fluorouracil