Preparation and distribution of 5-fluorouracil 125I sodium alginate-bovine serum albumin nanoparticles

AIM: To prepare 5-FU sodium alginate ¹²⁵I bovine serum albumin nanoparticles (BSA NP), to de-termine the radioactive count in different organs of rats at different time points after oral adminis-tration of 5-FU ¹²⁵I sodium alginate-BSA NP and to calculate the kinetic parameters of its metabolism.METHODS: Emulsion solidification method was used to prepare 5-FU ¹²⁵I sodium alginate-BSA NP, and to determine its diameter under trans-mission electronic microscope (TEM). Then the rate of NP and external drug releasing velocity were measured. Radioactive counting in different organs of rats wa s made after oral adminis-tration of the NP by GAMA Counter, and the ki-netic para meters of drug metabolism were calcu-lated by handling the data with the two-depart-ment model.RESULTS: The average arithmatic diameter of the NP was 166 nm ± 34 nm, the rate of 5-FU was 32.8% and the cumulative external releasing ra-tio amounted to 84.0% within 72 hours. The NP was mainly distributed in the liver, spleen, lungs and kidneys after NP oral administration to rats. The mic ro-radioautographic experiment showed that NP was distributed in the Kupffers cells of liver, liver parenchymal cells and the phagocytes of spleen and lungs. The kinetic pa-rameters of matabolism were: T_1/2 = 9.42 h, C_max =2.45 × 10⁷ Bq, T_max = 2.18 h, AUC = 148 × 10⁹ Bq.CONCLUSION: NP is difficult to pass through the blood-cerebral barrier,and ¹²⁵I sodium alginate-BSA NP enters the body circulation by gastroin testinal passage.