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Related Concept Videos

Drug Delivery: Overview01:16

Drug Delivery: Overview

705
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
705

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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
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Disulfide-Functionalized Covalent Organic Frameworks as Nanocarriers Realizing Programmed Cellular Internalization

Hao Ling1, Haozhou Shu1, Mengxing Zhang1

  • 1College of Polymer Science and Engineering, State Key Laboratory of Advanced Polymer Materials, Sichuan University, Chengdu 610065, P. R. China.

ACS Applied Materials & Interfaces
|November 20, 2025
PubMed
Summary
This summary is machine-generated.

Researchers engineered glutathione-sensitive covalent organic frameworks (COFs) with disulfide bonds. These nanocarriers improved drug delivery by enhancing cellular uptake and controlled release, showing promise for cancer therapy.

Keywords:
cellular uptakecovalent organic frameworkdisulfidedrug delivery

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Area of Science:

  • Materials Science
  • Nanotechnology
  • Biomedical Engineering

Background:

  • Covalent organic frameworks (COFs) show promise for drug delivery but face challenges with cell penetration and controlled release.
  • Developing stimuli-responsive nanocarriers is crucial for targeted and effective pharmaceutical applications.

Purpose of the Study:

  • To engineer glutathione-sensitive COFs (SSx-COFs) with tunable disulfide densities for enhanced bioactive molecule delivery.
  • To investigate the impact of disulfide incorporation on cellular uptake, drug release kinetics, and in vivo antitumor efficacy.

Main Methods:

  • Synthesis of SSx-COFs with varying disulfide densities by integrating disulfide motifs into COF backbones.
  • Characterization of COF nanocarriers for surface area, drug loading capacity, and disulfide content.
  • Evaluation of cellular uptake mechanisms via thiol-disulfide exchange and assessment of in vitro/in vivo drug release and antitumor activity.

Main Results:

  • SSx-COFs exhibited high surface areas and drug loading capacities.
  • Disulfide incorporation significantly enhanced COF cellular uptake and accelerated drug release, controllable by disulfide density.
  • Thiol-disulfide exchange mediated the enhanced cellular internalization pathway.
  • SS70-COF loaded with doxorubicin demonstrated potent in vitro and in vivo antitumor efficacy.

Conclusions:

  • Surface disulfide engineering is a viable strategy to enhance the intracellular delivery efficiency of nanocarriers.
  • Glutathione-sensitive SSx-COFs offer a promising platform for stimuli-responsive drug delivery systems.
  • This approach provides valuable insights for designing next-generation nanomedicines for cancer therapy.