4.8 Article

Modifying mesoporous silica nanoparticles to avoid the metabolic deactivation of 6-mercaptopurine and methotrexate in combinatorial chemotherapy

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NANOSCALE
卷 5, 期 14, 页码 6249-6253

出版社

ROYAL SOC CHEMISTRY
DOI: 10.1039/c3nr00227f

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  1. Beijing area major laboratory of peptide and small molecular drugs
  2. PHR (IHLB)
  3. NSFC [21171120, 81172930]
  4. Beijing Natural Science Foundation [7132020]
  5. Project for Science and Technology Development, Beijing Commission of Education [SQKM201210025007]

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Mesoporous silica nanoparticles with amino and thiol groups (MSNSN) were prepared and covalently modified with methotrexate and 6-mercaptopurine to form 6-MP-MSNSN-MTX. In the presence of DTT, 6-MP-MSNSN-MTX gradually releases 6-MP. In rat plasma, 6-MP-MSNSN-MTX effectively inhibits the metabolic deactivation of 6-MP and MTX. 6-MP-MSNSN-MTX could be an agent for long-acting chemotherapy.

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