Nucleus‐Targeting Gold Nanoclusters for Simultaneous In Vivo Fluorescence Imaging, Gene Delivery, and NIR‐Light Activated Photodynamic Therapy

Abstract

The nucleus is one of the most important cellular organelles and molecular anticancer drugs, such as cisplatin and doxorubicin, that target DNA inside the nucleus, are proving to be more effective at killing cancer cells than those targeting at cytoplasm. Nucleus‐targeting nanomaterials are very rare. It is a grand challenge to design highly efficient nucleus‐targeting multifunctional nanomaterials that are able to perform simultaneous bioimaging and therapy for the destruction of cancer cells. Here, unique nucleus‐targeting gold nanoclusters (TAT peptide–Au NCs) are designed to perform simultaneous in vitro and in vivo fluorescence imaging, gene delivery, and near‐infrared (NIR) light activated photodynamic therapy for effective cancer cell killing. Confocal laser scanning microscopy observations reveal that TAT peptide–Au NCs are distributed throughout the cytoplasm region with a significant fraction entering into the nucleus. The TAT peptide–Au NCs can also act as DNA nanocargoes to achieve very high gene transfection efficiencies (≈81%) in HeLa cells and in zebrafish. Furthermore, TAT peptide–Au NCs are also able to sensitize formation of singlet oxygen (1O2) without the co‐presence of organic photosensitizers for the destruction of cancer cells upon NIR light photoexcitation.

Bio‐Conjugated Advanced Materials for Targeted Disease Theranostics

“…AuNPs have been extensively used as a core for coating targeting peptides . Lee and co‐workers attached RGD (targets inflammation) to Au half‐shell nanoparticles containing methotrexate (MTX, most widely used RA therapeutic) as an improved photo‐/chemotherapy agent for the treatment of rheumatoid arthritis (RA) in collagen‐induced arthritic (CIA) mice.…”

Advances in Stimulus‐Responsive Polymeric Materials for Systemic Delivery of Nucleic Acids

“…Vankayala et al reported novel and unique multifunctional gold nanoclusters with nuclear targeting properties. This theranostic nanoplatform was designed to perform simultaneous fluorescence imaging, gene delivery and long (850–1100 nm) NIR light-activated photodynamic therapy for the destruction of cancer cells [98]. The percentage of gene transfection using these multifunctional gold nanoclusters was nearly 3.2-fold higher than that obtained using the most commonly adopted LP2000 liposome gene carrier with NIR light irradiation.…”

Ethylene glycol-mediated synthetic route for production of luminescent silicon nanorod as photodynamic therapy agent

“…Alternative nanostructure hosts containing classical organic PSs have demonstrated improved water solubility and stability; however, most of these methods use nonfunctional polymer-based or silica nanomaterials as carriers, risking the leakage of PS payload from the carriers into the body before reaching their target tumor [11,12]. Nanomaterials, such as TiO 2 [13], tin tungstate nanoparticles [14], ZnO [15], metal nanocluster [16], Cdquantum dots [17], carbon dots [18][19][20], and black phosphorus nanosheets [21], which intrinsically produce 1 O 2 when photoexcited, can overcome these shortcomings. However, concerns regarding biocompatibility and biodegradability of such nanomaterials have hindered their clinical translation.…”