A Single Molecule Drug Targeting Photosensitizer for Enhanced Breast Cancer Photothermal Therapy

Abstract

Targeting is one of the most important strategies for enhancing the efficacy of cancer photothermal therapy (PTT) and reducing damage to surrounding normal tissues. Compared with the traditional targeting approaches, the active targeting of breast cancer cells in PTT using chemotherapeutic drugs, such as tamoxifen (TAM), in combination with single‐molecule photothermal photosensitizers has superior selectivity and therapeutic effects. However, single‐molecule drug‐targeting photosensitizers for improved PTT efficacy are not widely reported. Accordingly, herein, a near‐infrared induced small‐molecule photothermal photosensitizer (CyT) is developed that actively targets the estrogen receptors (ERs) of breast cancer cells as well as targets mitochondria by structure‐inherent targeting. Cell uptake and cytotoxicity studies using different types of cells show that CyT enhances the efficiency of TAM‐based PTT by targeting ER‐overexpressing breast cancer cells and selectively killing them. In vivo experiments demonstrate that CyT can be used as a photothermal agent for fluorescence imaging‐guided PTT. More importantly, the intravenous injection of CyT results in better targeting and efficiency of tumor inhibition compared with that achieved with the TAM‐free control molecule Cy. Thus, the study presents an excellent small‐molecule photothermal agent for breast cancer therapy with potential clinical application prospects.

Highly stable organic photothermal agent based on near-infrared-II fluorophores for tumor treatment

“…In addition, the photothermal conversion efficiency was measured as 50.5% (Additional file 1: Fig. S6c-f ), higher than that of most photothermal agents [39][40][41][42][43]. In addition, NIR998 NPs (20 μM) solution showed a high temperature increase up to 26 °C under irradiation (808 nm, 0.5 W cm −2 , 6 min), which helped to effectively suppress tumor growth, indicating that NIR998 NPs could serve as promising photothermal agent for tumor photothermal therapy.…”

Design Principles Governing the Development of Theranostic Anticancer Agents and Their Nanoformulations with Photoacoustic Properties

“…For instance, Yang et al developed a cyanine-based theranostic agent that contains tamoxifen. In this specific example, the linker consists of a 1,4-disubstituted triazole ring followed by an alkyl chain serving as spacer to fulfill molecular co-delivery requirements [120]. Another example by Yang et al is a conjugate of a heptamethine cyanine dye-IR 78, tethered by an ether bond with the flavonoid-based natural product genistein [121].…”

Plasmonic gold nanoagents for cancer imaging and therapy

“…PT agents are accumulated in tumor tissues using targeted recognition techniques, and light energy is converted into heat energy to kill localized tumor cells under the irradiation of external NIR light. [43,70,71] Goldbased nanomaterials are excellent PT agents because of A-D) Reproduced with permission. [46] Copyright 2020, Ivyspring International Publisher.…”