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Issue 4, 2019
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Design of 5-fluorouracil (5-FU) loaded, folate conjugated peptide linked nanoparticles, a potential new drug carrier for selective targeting of tumor cells

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Abstract

In the present investigation folate peptide (FA-Pep) conjugated 5-fluorouracil (5-FU) loaded nanoparticles were synthesized and their tumor targeting potentiality was monitored by different in vitro and in vivo techniques. FA-Pep-1 and FA-Pep-2 were synthesized and radiolabeled with 99mTc(CO)3(H2O)3. 99mTc(CO)3-FA-Pep-1 exhibited promising tumor uptake in an in vivo model (nude mice bearing HeLa cell xenograft and Balb/c mice bearing B16F10 melanoma tumor) as compared to 99mTc(CO)3-FA-Pep-2. FA-Pep-1 was then conjugated with 5-FU-NPs (118 ± 4.3), as confirmed by the XPS study. These showed promising cytotoxic and apoptotic potential in B16F10 cell lines as compared to free 5-FU and unconjugated 5-FU-NPs. In vivo biodistribution and gamma-scintigraphy showed good accumulation of peptide conjugated NPs in the tumor region. Therapeutic efficacy studies in B16F10 tumor xenografts also exhibited substantial tumor growth inhibition. The above studies reveal that folate peptide conjugation may facilitate the tumor-targeting approach of 5-FU-NPs.

Graphical abstract: Design of 5-fluorouracil (5-FU) loaded, folate conjugated peptide linked nanoparticles, a potential new drug carrier for selective targeting of tumor cells

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Publication details

The article was received on 16 Nov 2018, accepted on 08 Mar 2019 and first published on 12 Mar 2019


Article type: Research Article
DOI: 10.1039/C8MD00565F
Citation: Med. Chem. Commun., 2019,10, 559-572

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    Design of 5-fluorouracil (5-FU) loaded, folate conjugated peptide linked nanoparticles, a potential new drug carrier for selective targeting of tumor cells

    J. Kazi, R. Mukhopadhyay, R. Sen, T. Jha, S. Ganguly and M. C. Debnath, Med. Chem. Commun., 2019, 10, 559
    DOI: 10.1039/C8MD00565F

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