Preprint Article Version 1 This version is not peer-reviewed

Preparation, Characterization, Cytotoxicity and Biological Evaluation of 99mTc-Doxorubicin-Epigallocatechingallate Functionalized Gold Nanoparticles as a New Generation of Theranostic Radiopharmaceutical

Version 1 : Received: 17 August 2018 / Approved: 18 August 2018 / Online: 18 August 2018 (08:32:59 CEST)

How to cite: Sakr, T.M.; Morsy, S.A.G.; Mahmoud, N.A.; Rashed, H.M.; El-Rehim, H.A.A.; Khoobchandani, M.; Katti, K.K.; Katti, K.V. Preparation, Characterization, Cytotoxicity and Biological Evaluation of 99mTc-Doxorubicin-Epigallocatechingallate Functionalized Gold Nanoparticles as a New Generation of Theranostic Radiopharmaceutical. Preprints 2018, 2018080331 (doi: 10.20944/preprints201808.0331.v1). Sakr, T.M.; Morsy, S.A.G.; Mahmoud, N.A.; Rashed, H.M.; El-Rehim, H.A.A.; Khoobchandani, M.; Katti, K.K.; Katti, K.V. Preparation, Characterization, Cytotoxicity and Biological Evaluation of 99mTc-Doxorubicin-Epigallocatechingallate Functionalized Gold Nanoparticles as a New Generation of Theranostic Radiopharmaceutical. Preprints 2018, 2018080331 (doi: 10.20944/preprints201808.0331.v1).

Abstract

Gold nanoparticles are currently used for the treatment of cancer through a myriad of modalities and delivery approaches. Conjugation of tumor imaging Single Photon Emitting Computed Tomographic (SPECT) radiopharmaceutical to gold nanoparticles will allow systemic targeting and imaging of cancer tissues simultaneously. In this study, gold nanoparticles (AuNPs) were prepared using Epigallocatechingallate (EGCG), loaded with doxorubicin (Dox), and characterized before and after doxorubicin conjugation. Cytotoxicity of EGCG-AuNPs and Dox-EGCG-AuNPs were evaluated against breast carcinoma (MCF-7) and hepatocellular carcinoma (HepG-2) cell lines demonstrating high cytotoxic effects of Dox-EGCG-AuNPs against both cell lines. Doxorubicin was radiolabeled with 99mTc and our new approach has optimized various labeling conditions resulting in a radiochemical yield of 93.5 ± 2.04%. Biodistribution of 99mTc-Dox-EGCG-AuNPs was studied in normal and tumor bearing mice following I.V. and intratumoral injections at different time intervals. Results showed high uptake of the intravenously injected 99mTc-Dox-EGCG-AuNPs in tumor tissue (22.45 %ID/g at 2 h). In addition, localized intratumoral injection of 99mTc-Dox-EGCG-AuNPs showed extremely high levels of uptake in tumor (80.22 %ID/g at 15 min) with high retention for extended periods post injection. Our results present prospects for the utility of 99mTc-Dox-EGCG-AuNPs as a multiplexed theranostic agent through SPECT imaging of tumor tissue and therapy through photothermal destruction of cancer tissue through the application of exogenous laser lights as well as through tyrosine phosphatases inhibitor (through EGCG), and topoisomerase II inhibitor (through doxorubicin) effects.

Subject Areas

gold nanoparticles; EGCG; doxorubicin; radiolabeling; theranostics

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