Folate-conjugated albumin nanoparticles for rheumatoid arthritis-targeted delivery of etoricoxib

被引:55
作者
Bilthariya, Upasana [1 ]
Jain, Nivrati [1 ]
Rajoriya, Vaibhav [1 ]
Jain, Ashish Kumar [1 ]
机构
[1] ADINA Inst Pharmaceut Sci, Div Pharmaceut, Sagar 470002, Madhya Pradesh, India
关键词
Activated macrophages targeting; etoricoxib; folate conjugation; inflammation screening; rheumatoid arthritis; SYNOVIAL TISSUE; PROTEIN; MACROPHAGES; CYCLOOXYGENASE-2; ENDOCYTOSIS; EXPRESSION; CELLS; BETA;
D O I
10.3109/03639045.2013.850705
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
Objective: The present study discusses folic acid-etoricoxib-bovine serum albumin nanoparticles (F-ETX-NPs) using folic acid as an over expressed folate receptor ligand for activated macrophages in targeting of rheumatoid arthritis. Materials and methods: For this purpose etoricoxib-loaded BSA nanoparticles (ETX-NPs) were prepared by desolvation method and activated folic acid conjugation with free amine group of BSA was confirmed by FTIR study and zeta potential measurements. Results: The F-ETX-NPs showed spherical in shape with 215.8 +/- 3.2 nm average size +/- 7.8 mV zeta potential, 72 +/- 1.3% etoricoxib entrapment efficiency and showed 93.1 +/- 2.2% cumulative etoricoxib release upto 72 h. The etoricoxib concentration from F-ETX-NPs was found to be 9.67 +/- 0.34 mu g/g in inflamed joint after 24 h administration revealed remarkably targeting potential to the activated macrophages cells and keep at a high level during the experiment. Discussion and conclusion: These results suggest that F-ETX-NPs are potentially vector for activated macrophages cells targeting of rheumatoid arthritis.
引用
收藏
页码:95 / 104
页数:10
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