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Abstract <p>Recently well designed multifunctional nanoparticles capable of delivering drugs in a controlled manner with low toxicity and high target specificity upheld a significant role in tumour therapy. Here, safe and controlled drug delivery of anti-melanoma drug dacarbazine (DTIC) is attained in malignant melanoma (A375) cells using metal organic frameworks (MOFs) based drug delivery systems. Green fluorescent crystalline fluorescein 5-isothiocyanate (FITC) labelled Zeolitic imidazolate framework-8 (ZIF-8) nanoparticles having a particle size (70&#xa0;nm) within the biological regime, synthesised through solvothermal approach was employed as the carrier nanoparticles of the anti-melanoma drug dacarbazine. The ZIF-8 carrier nanoparticles were found to be cytocompatible as well as hemocompatible and also possess 62% drug encapsulation efficiency. Acidic pH sensitive decomposition of the nanoparticles and the subsequent delivery of the drug dacarbazine was investigated through the drug release studies. The maximum drug release was observed (around 80% in 24&#xa0;h) at a pH value of 5 which is consistent with the acidic pH observed in the endosomes or lysosomes thereby enabling selective intra cellular drug release. The encapsulation of the drug in ZIF-8 helps to improve the bioavailability of the drug at the target site as confirmed from the MTT studies. The apoptotic studies confirms the potential of the nanoparticles against A375 human melanoma cells. The IC<sub>50</sub> value of the nanoparticles in A375 cells was found to be 120.12 ± 3.8&#xa0;µg/mL, 42.29 ± 2.95&#xa0;µg/mL and 12.27 ± 2.77&#xa0;µg/mL for 24&#xa0;h, 48&#xa0;h and 72&#xa0;h incubation time respectively. The apoptotic potential of the DTIC loaded nanocarriers was established in human malignant melanoma cells (A375) through various <i>in vitro</i> studies. Continued research using <i>in vivo</i> methods can further refine the results and expand their clinical applications. Our potential results upheld the fact that the FITC labelled DTIC@ZIF-8 nanoparticles can be utilized as a novel candidate for pH-triggered drug delivery applications in the treatment of malignant melanoma.</p> Graphical Abstract <p>PH sensitive drug release of drug loaded in the nanocarrier.</p> <p><i>[Reused from Arun Unnikrishna pillai, Rajeswari Sreeja, Monisha Mohanan Sailaja, Annie Abraham, Chapter 3 – Metal Organic Framework (MOF) based nanostructures for light mediated cancer therapy, Editor(s): Raji Vijayamma, Nandakumar Kalarikkal, Sabu Thomas, In Nanotechnology in Biomedicine, Nanostructured Materials for Biomedical Applications, Elsevier, 2024, Pages 73-88, ISBN 9780323908382]</i></p> <p></p>

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pH Sensitive Drug Release of FITC Labelled Dacarbazine Loaded ZIF-8 Nanoparticles and the Investigation of Its Anti-melanoma Efficacy In vitro

  • 期刊论文

  • 发表日期：

    2026年5月8日

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  • U. Arun,
  • R. Sreeja,
  • Annie Abraham

摘要

Abstract

Recently well designed multifunctional nanoparticles capable of delivering drugs in a controlled manner with low toxicity and high target specificity upheld a significant role in tumour therapy. Here, safe and controlled drug delivery of anti-melanoma drug dacarbazine (DTIC) is attained in malignant melanoma (A375) cells using metal organic frameworks (MOFs) based drug delivery systems. Green fluorescent crystalline fluorescein 5-isothiocyanate (FITC) labelled Zeolitic imidazolate framework-8 (ZIF-8) nanoparticles having a particle size (70 nm) within the biological regime, synthesised through solvothermal approach was employed as the carrier nanoparticles of the anti-melanoma drug dacarbazine. The ZIF-8 carrier nanoparticles were found to be cytocompatible as well as hemocompatible and also possess 62% drug encapsulation efficiency. Acidic pH sensitive decomposition of the nanoparticles and the subsequent delivery of the drug dacarbazine was investigated through the drug release studies. The maximum drug release was observed (around 80% in 24 h) at a pH value of 5 which is consistent with the acidic pH observed in the endosomes or lysosomes thereby enabling selective intra cellular drug release. The encapsulation of the drug in ZIF-8 helps to improve the bioavailability of the drug at the target site as confirmed from the MTT studies. The apoptotic studies confirms the potential of the nanoparticles against A375 human melanoma cells. The IC50 value of the nanoparticles in A375 cells was found to be 120.12 ± 3.8 µg/mL, 42.29 ± 2.95 µg/mL and 12.27 ± 2.77 µg/mL for 24 h, 48 h and 72 h incubation time respectively. The apoptotic potential of the DTIC loaded nanocarriers was established in human malignant melanoma cells (A375) through various in vitro studies. Continued research using in vivo methods can further refine the results and expand their clinical applications. Our potential results upheld the fact that the FITC labelled DTIC@ZIF-8 nanoparticles can be utilized as a novel candidate for pH-triggered drug delivery applications in the treatment of malignant melanoma.

Graphical Abstract

PH sensitive drug release of drug loaded in the nanocarrier.

[Reused from Arun Unnikrishna pillai, Rajeswari Sreeja, Monisha Mohanan Sailaja, Annie Abraham, Chapter 3 – Metal Organic Framework (MOF) based nanostructures for light mediated cancer therapy, Editor(s): Raji Vijayamma, Nandakumar Kalarikkal, Sabu Thomas, In Nanotechnology in Biomedicine, Nanostructured Materials for Biomedical Applications, Elsevier, 2024, Pages 73-88, ISBN 9780323908382]