Drug molecules bridge with small gatekeeper to co-block mesoporous silica nanoparticles for drug delivery.

Colloids Surf B Biointerfaces

School of Chemical Engineering, Sichuan University, Chengdu 610065, China. Electronic address:

Published: May 2022

In this study, a filter-like blocking system based on MSN with small gatekeeper 5- mercapto-2 nitrobenzoic acid (MNBA) has developed. The MNBA grafted nanoparticle MSN-SS-MNBA shows excellent blocking performance with negligible leakage when loaded with doxorubicin (DOX), and the release profiles illustrate stimuli-responsive property when triggered by GSH. Viability experiments indicate that MSN-SS-MNBA has obvious inhibition for both Hela cells and HCT116 cells, while showing good biocompatibility for L929 cells, which suggests that the modified MNBA has a synergistic effect on cancer cells-killing. Since the small grafted molecule MNBA cannot block the channels of MSN via self-assembly, a filter-like blocking model that the loaded drug bridged with modified MNBA to fulfill the blocking process is proposed. The novel blocking strategy provides a new possible way for pore blocking, and the small nanovalve can be used as synergistic molecule for cancer therapy.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.colsurfb.2022.112350DOI Listing

Publication Analysis

Top Keywords

small gatekeeper
8
filter-like blocking
8
modified mnba
8
blocking
6
mnba
5
drug molecules
4
molecules bridge
4
small
4
bridge small
4
gatekeeper co-block
4

Similar Publications

Epidermal growth factor receptor (EGFR) is a highly expressed driver of many cancers, yet the utility of EGFR inhibitors is limited to cancers that harbor sensitizing mutations in the EGFR gene due to dose limiting toxicities. Rather than conventionally blocking the kinase activity of EGFR, we sought to reduce its transcription as an alternative approach to broaden the therapeutic window for EGFR inhibitors targeting wildtype or mutant EGFR. We found that YES1 is highly expressed in triple negative breast cancer (TNBC) and drives cell growth by elevating EGFR levels.

View Article and Find Full Text PDF

Metastatic cancer cells undergo metabolic reprogramming, which involves changes in the metabolic fluxes, including endocytosis, nucleocytoplasmic transport, and mitochondrial metabolism, to satisfy their massive demands for energy, cell division, and proliferation compared to normal cells. We have previously demonstrated the ability of two different types of compounds to interfere with linchpins of metabolic reprogramming, Pitstop-2 and 1,6-hexanediol (1,6-HD). 1,6-HD disrupts glycolysis enzymes and mitochondrial function, enhancing reactive oxygen species production and reducing cellular ATP levels, while Pitstop-2 impedes clathrin-mediated endocytosis and small GTPases activity.

View Article and Find Full Text PDF

A Patient-Oriented Implementation Strategy for a Perioperative mHealth Intervention: Feasibility Cohort Study.

JMIR Perioper Med

January 2025

Societal Participation & Health, Amsterdam Public Health, Amsterdam, The Netherlands.

Background: Day surgery is being increasingly implemented across Europe, driven in part by capacity problems. Patients recovering at home could benefit from tools tailored to their new care setting to effectively manage their convalescence. The mHealth application ikHerstel is one such tool, but although it administers its functions in the home, its implementation hinges on health care professionals within the hospital.

View Article and Find Full Text PDF

Background: The majority of functional ischemia tests in patients with suspected chronic coronary syndromes (CCS) yield normal results. Implementing gatekeepers for patient preselection, such as pretest probability (PTP) and/or coronary artery calcium score (CACS), could reduce the number of normal scan results, radiation exposure and costs. However, the efficacy and safety of these approaches remain unclear.

View Article and Find Full Text PDF

When companies are uncertain about the potential of a new formulation to be bioequivalent to a Reference product, it is common practice to carry out downsized pilot studies as a gatekeeping in vivo strategy to decide whether to move forward or not with a full-size pivotal study. However, due to the small study size, these studies are inarguably more sensitive to variability. To address and mitigate the uncertainty of the conclusions of pilot studies concerning the maximum observed concentration (C), the factor was proposed as an alternative approach to the average bioequivalence statistical methodology.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!