Study on Distribution in vivo and Pharmacodynamics of Prodrug Folate-Bovine Serum Albumin-5-Fluorouracil Nanoparticles
HE Lian-qin，ZHU Liang*
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Guangdong Pharmaceutical University， Guangzhou 510006， China
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Received
Revised
Published
2012-01-01
2012-01-01
2012-01-01
Issue Date
2010-01-15
Abstract
OBJECTIVE To investigate the distribution in vivo and pharmacodynamics of prodrug folate-bovine serum albumin-5-fluorouracil nanoparticles in mice．METHODS The H22 hepatoma cells solid tumor mouse model was established. The effect of Folate-BSA-5-Fu nanoparticles (high， medium and low) on tumor growth conditions in the tumor-bearing mice were studied，and compared with bovine serum albumin-5-fluorouracil (BSA-5-Fu) nanoparticles group， folate blocking group (free folate+folate-BSA-5-Fu nanoparticles)， positive 5-fluorouracil group and negative saline group.After intraperitoneal injection, the distribution of experimental group loaded calcein nanoparticles were determined by fluorospectrophotometry.RESULTS The tumor growth in tumor-bearing mice was the slowest in high dose folate-BSA-5-Fu nanoparticles group. The inhibition rate was the highest after intraperitoneal injection. The inhibition rate of folate-BSA-5-Fu nanoparticles were higher than that of BSA-5-Fu nanoparticles. After coadministration of 1 mmol·L-1 exogenous folate， the inhibition rate of folate-BSA-5-Fu nanoparticles were decreased significantly. The inhibition rate of 5-Fu-sol was higher than that of BSA-5-Fu nanoparticles. The distribution content in vivo of folate-BSA-5-Fu loaded calcein nanoparticles were higher than that of BSA-5-Fu loaded calcein nanoparticles.CONCLUSION Folate - bovine serum albumin-5 - fluorouracil was a potential anti-tumor prodrug and it can be targeted at the high expression of folate receptor tumor.
HE Lin-qin;ZHU Ling.
Study on Distribution in vivo and Pharmacodynamics of Prodrug Folate-Bovine Serum Albumin-5-Fluorouracil Nanoparticles[J]. Chinese Pharmaceutical Journal, 2010, 45(2): 107-110
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References
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