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Preparation and characterisation of zinc diethyldithiocarbamate–cyclodextrin inclusion complexes for potential lung cancer treatment

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posted on 2024-01-08, 14:47 authored by Ayşe Kaya, Basel Arafat, Havovi Chichger, Ibrahim Tolaymat, Barbara Pierscionek, Mouhamad Khoder, Mohammad Najlah
Zinc diethyldithiocarbamate (Zn (DDC)2), a disulfiram metabolite (anti-alcoholism drug), has shown a strong anti-cancer activity in vitro. However, its application was limited by its low aqueous solubility and rapid metabolism. In this study, the solubility enhancement of Zn (DDC)2 is investigated by forming inclusion complexes with cyclodextrins. The inclusion complexes were prepared using two different types of beta-cyclodextrins, SBE-CD and HP-CD. Phase solubility diagrams for the resulting solutions were assessed; subsequently, the solutions were freeze-dried for further characterisation studies using DSC, TGA, XRD, and FTIR. The cytotoxic activity of the produced inclusion complexes was evaluated on human lung carcinoma cells using the MTT assay. The solubility of Zn (DDC)2 increased significantly upon adding beta-cyclodextrins, reaching approximately 4 mg/mL for 20% w/w CD solutions. The phase solubility diagram of Zn (DDC)2 was of the Ap-type according to the Higuchi and Connors model. Characterisation studies confirmed the inclusion of the amorphous drug in the CD-Zn (DDC)2 complexes. The cytotoxicity of Zn (DDC)2 was enhanced 10-fold by the inclusion complexes compared to the free drug. Overall, the resulting CD-Zn (DDC)2 inclusion complexes have a potential for treatment against lung cancer.

History

Refereed

  • Yes

Volume

16

Issue number

1

Publication title

Pharmaceutics

ISSN

1999-4923

Publisher

MDPI AG

File version

  • Published version

Language

  • eng

Affiliated with

  • School of Allied Health Outputs