Synthesis of Carbohydrate Capped Silicon Nanoparticles and their Reduced Cytotoxicity, In Vivo Toxicity, and Cellular Uptake

Abstract

The development of smart targeted nanoparticles (NPs) that can identify and deliver drugs at a sustained rate directly to cancer cells may provide better efficacy and lower toxicity for treating primary and advanced metastatic tumors. Obtaining knowledge of the diseases at the molecular level can facilitate the identification of biological targets. In particular, carbohydrate‐mediated molecular recognitions using nano‐vehicles are likely to increasingly affect cancer treatment methods, opening a new area in biomedical applications. Here, silicon NPs (SiNPs) capped with carbohydrates including galactose, glucose, mannose, and lactose are successfully synthesized from amine terminated SiNPs. The MTT [3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide] analysis shows an extensive reduction in toxicity of SiNPs by functionalizing with carbohydrate moiety both in vitro and in vivo. Cellular uptake is investigated with flow cytometry and confocal fluorescence microscope. The results show the carbohydrate capped SiNPs can be internalized in the cells within 24 h of incubation, and can be taken up more readily by cancer cells than noncancerous cells. Moreover, these results reinforce the use of carbohydrates for the internalization of a variety of similar compounds into cancer cells.

Presence of an Immune System Increases Anti‐Tumor Effect of Ag Nanoparticle Treated Mice

“…As our studies are performed on the short‐term exposure (24 h) of cells to NPs, this does not resemble the in vivo situation, where upon peritumoral administration of the NPs, the cancer cells will be exposed to the NPs for longer time periods. The 24 h exposure time has been chosen in line with literature, where cellular NP exposure is often 24 h, mainly driven by the fact that for efficient cellular NP uptake, cells should have undergone one cell cycle . As for different cell types, the cell cycle duration can differ quite a bit, a time period of 24 h is chosen as a mean value.…”

Glyco-functionalised quantum dots and their progress in cancer diagnosis and treatment

“…Visualisation imaging of SiNPs in MCF-7 human breast cancer cells showed the fluorescence was distributed throughout the cytoplasm of these cells. Later the same research group prepared SiNPs capped with different carbohydrates including galactose, glucose, mannose, and lactose from amine terminated SiNPs [64,75]. The MTT analysis showed an extensive reduction in toxicity of SiNPs by functionalizing with carbohydrate moiety in vitro.…”

Mannose and Mannose‐6‐Phosphate Receptor–Targeted Drug Delivery Systems and Their Application in Cancer Therapy

“…Many of the current available therapies are still inadequate and, despite the last advances in understanding biological mechanisms behind cancer progression, many patients have relapses due to the proliferation of residual malignant cells [2] or because cancer cells mutate and develop resistance, which renders also the most recent treatments ineffective. [3] Moreover, the shortage of selective delivery of anti-cancer drugs to tumor tissues is still one of the major limitations to overcome in order to reduce toxicity of chemotherapeutics and increase the efficiency of many treatments. [4]…”

“…Therefore, the need of finding new potential targets to address anticancer drugs is urgent, and in this regard would be desirable to take especially biological markers into account which have a lower tendency to mutate. [3] Moreover, combining conventional chemotherapeutic cancer therapy with more innovative approaches such as immunotherapy or theragnostics would potentially result in a more durable remission. [5]…”

“…Since lectin type receptors are over-expressed in many tumors, they can be used to selectively target and deliver drugs, or diagnostic probes to cancer cells by receptor-mediated endocytosis, providing better efficacy and lower toxicity in healthy tissues. [3] Moreover, the presence of mannose receptor (MR) on the surface of professional antigen presenting cells (APCs) involved in immune responses, such as macrophages (MCs) and dendritic cells (DCs), would allow their targeting and subsequent modulation, in order to induce a specific and long-lasting anticancer response. [6]…”