Peptide conjugated water-soluble chitosan for green synthesis of gold nanoparticles as radiopharmaceuticals

Name: Theeranan Tangthong

LCSH: Kasetsart University -- Dissertations. Ph.D. (Nanomaterials Science) 2021

Classification :.LCCS: RS201.N35

LCSH: Kasetsart University. -- Department of Materials Science -- Dissertations

LCSH: Radiopharmaceuticals

LCSH: Nanoparticles

LCSH: Chitosan

LCSH: Gold

LCSH: Peptides

LCSH: Prostate -- Cancer

LCSH: Bioconjugates

Abstract: Gold nanoparticles (AuNPs) have several applications including in medicine. Considering cancer is one of the most common diseases for men and women, new treatments and more specific and effective drugs, which cause less side effects, have been actively pursued. Among them, gold-198 can be engineered as theranostic agent, working as contrast (exploiting gamma emission) and treatment agents (beta emission). Rapid one-pot synthesis of AuNPs as target therapeutic agent is a way to efficiently create targeted AuNPs as well as its analogue radioactive form as a ready-to-used therapeutic agent. To improve antioxidant activity including reducing capacity of water-soluble chitosan (WSC), anchoring the polyphenolic group and targeting peptide onto WSC nanocolloids are our strategy to prepare an effective reducing, stabilizing and targeting agent for a rapid one-pot synthesis of AuNPs. In this view point, bio-conjugated WSC gallate nanocolloids was prepared by functionalizing gallic acid (GA) onto WSC and further conjugating with DOTA-Bombesin (DBBN) peptides that they have demonstrated high affinity toward gastrin-releasing peptide (GRP) receptors in vivo that are overexpressed in prostate, breast, and small-cell lung carcinoma. The DBBN content on the WSC-DBBN and WSCGA-DBBN sample were ~6% and ~27 %w/w, respectively. The WSCGA-DBBN nanocolloids exhibited almost 12 times more enriched antioxidant activity than WSC. They showed high efficiency to rapid one-pot synthesize stable WSC-DBBN-AuNPs and WSCGA-DBBN with a desirable hydrodynamic diameter range of 60-70 and 40-60 nm, respectively. The obtained AuNPs were stable over 4 days after preparation and ~3 days after subjecting to all relevant biological fluids. The study proves that DBBN peptide anchoring on the WSC and WSCGA capped on AuNPs play an important role for targeting as an evidence of the cellular internalization of AuNPs showing more significant into PC-3 than LNCaP cells. Accordingly, the targeted WSC-DBBN-AuNPs and WSCGADBBN-AuNPs nanoplatform also exhibited superior therapeutic treatment of the PC-3 over LNCaP prostate cancer cells. Moreover, we have demonstrated a facile method to efficiently produce radioactive isotopes, ready-to-used in cancer theragnostic. The interaction of WSCDBBN and WSCGA-DBBN with a Au-198 gold precursor affords 198AuNPs as the beta emissions of Au-198 provide unique advantages for tumor therapy while gamma rays are used for the quantitative estimation of 198AuNPs. Our observation is one of a promising and practical way to prepare targeted AuNPs therapeutic agent for a model prostate cancer cell treatment and for further enhancing therapeutic efficacy and minimize side effects of anticancer drugs.

Kasetsart University. Office of the University Library

Address: Bangkok

Email: tdckulib@ku.ac.th

Name: Wanvimol Pasanphan

Role: Thesis Advisor

Created: 2021

Modified: 2025-07-12

Issued: 2025-07-12

วิทยานิพนธ์/Thesis

application/pdf

URL: https://www.lib.ku.ac.th/KUthesis/2564/theeranan-tan-all.pdf

CallNumber: RS201.N35 .T44

eng

DegreeName: Doctor of Philosophy

Level: Doctoral Degraee

Descipline: Nanomaterials Science

Grantor: Kasetsart University

©copyrights Kasetsart University

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