Radiotracer labeled thymohydroquinyl gallate capped gold nanoparticles as a theranostic radiopharmaceutical for targeted antineoplastic and bioimaging.

Munaza BATOOL; Batool FATIMA; Dilshad HUSSAIN; Rubaida MAHMOOD; Muhammad IMRAN; Saeed AKHTER; Muhammad Saqib KHAN; Saadat MAJEED; Muhammad NAJAM-UL-HAQ

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Radiotracer labeled thymohydroquinyl gallate capped gold nanoparticles as a theranostic radiopharmaceutical for targeted antineoplastic and bioimaging.

Author: Munaza BATOOL ¹ ; Batool FATIMA ¹ ; Dilshad HUSSAIN ² ; Rubaida MAHMOOD ³ ; Muhammad IMRAN ⁴ ; Saeed AKHTER ³ ; Muhammad Saqib KHAN ³ ; Saadat MAJEED ⁵ ; Muhammad NAJAM-UL-HAQ ⁵
Author Information

1. Department of Biochemistry, Bahauddin Zakariya University, Multan, 60800, Pakistan.
2. HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
3. MINAR Cancer Hospital, Multan, Multan 60000, Pakistan.
4. Biochemistry Section, Institute of Chemical Sciences, University of Peshawar, Peshawar, Pakistan.
5. Institute of Chemical Sciences, Bahauddin Zakariya University, Multan, 60800, Pakistan.
Publication Type:Journal Article
Keywords: Cancer theranostics; Gallic acid; Gold nanoparticles; Targeted drug delivery; Thymoquinone
From: Journal of Pharmaceutical Analysis 2025;15(4):100965-100965
CountryChina
Language:English
Abstract: Thymoquinone (Tq) and gallic acid (GA) are known for counter-tumorigenic characteristics. GA inhibits cancer cell proliferation by interfering with many apoptotic signaling pathways, producing more reactive oxygen species (ROS), focusing on the cell cycle, and suppressing the expression of oncogenes and matrix metalloproteinases (MMPs). In this study, thymoquinone (after reducing to thymohydroquinone) and gallic acid are esterified to form thymohydroquinyl gallate (a prodrug). Thymohydroquinyl gallate (THQG) possesses enhanced antineoplastic efficacy and targeted delivery potential. The chemical and spectroscopic analysis confirms ester synthesis. Gold nanoparticles (AuNPs) are employed as nanocarriers due to their physicochemical and optical characteristics, biocompatibility, and low toxicity. As an efficient drug transporter, gold nanoparticles (AuNPs) shield conjugated drugs from enzymatic digestion. The prodrug acts as a reducing agent for Au metal atoms and is loaded onto it after reduction. The nano drug is radiolabeled with ^99mTc and ¹³¹I to monitor the drug biodistribution in animals using a gamma camera and single-photon emission computerized tomography (SPECT). ¹³¹I is an antineoplastic that helps enhance the drug's efficiency. Chromatographic results reveal promising radiolabeling percentages. In vitro, drug release shows sustained release at pH⁓5.8. In vitro 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) cytotoxicity assay reveals drug potency on CAL 27 and MCF 7 cell lines.