Active targeted ligand-aza-BODIPY conjugate for near-infrared photodynamic therapy in melanoma

Ng, Shie Yin and Kamkaew, Anyanee and Fu, Nanyan and Kue, Chin Siang and Chung, Lip Yong and Kiew, Lik Voon and Wittayakun, Jatuporn and Burgess, Kevin and Lee, Hong Boon (2020) Active targeted ligand-aza-BODIPY conjugate for near-infrared photodynamic therapy in melanoma. International Journal of Pharmaceutics, 579. ISSN 0378-5173, DOI

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Active targeting compound, a non-iodinated derivative of IK-IK-I-2-azaBODIPY (1a) was previously reported to preferentially bind melanoma over healthy cells. In this study, we evaluate the photodynamic therapy (PDT) efficiency on melanoma cells of 1a, together with its reversed sequence compound KI-KI-I-2-azaBODIPY (1b) and a non-targeted control I-2-azaBODIPY-NH2 (2). All three test compounds possess absorption wavelengths in the near-infrared (NIR) region (lambda(max) between 678 and 687 nm) which alleviate melanin interference and allow deeper tissue penetration. In vitro studies revealed 1a and 1b are promising photosensitizers with enhanced singlet oxygen generation, have increased uptake by B16-F10 melanoma cells via clathrin-mediated endocytosis and good photocytotoxic efficacies. Ex vivo biodistribution assays showed both 1a and 1b accumulated in the tumour. In B16-F10 tumour bearing-C57BL/6 mice, 10 mg/kg of 1b and light irradiation was found to reduce tumour volume by up to 23% at day-3. Doubling the dosage of 1b (20 mg/kg) enhanced the antitumour effect, showing 96% maximum tumour volume reduction at day-7 and tumour growth suppression for up to 12 days.

Item Type: Article
Funders: Postgraduate Research Grant (PPP) (PG222-2016A), Fujian Provincial Natural Science Foundation, P.R. China (2017J01577), Thailand Research Fund (TRF), Office of the Higher Education Commission (OHEC) Grant (MRG6180030)
Uncontrolled Keywords: Photodynamic therapy; Targeting; Small molecule ligand; Aza-BODIPY; Cancer; Melanoma
Subjects: R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Divisions: Faculty of Medicine
Faculty of Pharmacy
Depositing User: Ms Zaharah Ramly
Date Deposited: 17 Jan 2023 06:30
Last Modified: 17 Jan 2023 06:30

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