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Related Concept Videos

Drug-Receptor Bonds01:25

Drug-Receptor Bonds

Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
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Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
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Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...

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Related Experiment Video

Updated: Jun 6, 2026

Synthesis of Immunotargeted Magneto-plasmonic Nanoclusters
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"Hook&Loop" multivalent interactions based on disk-shaped nanoparticles strengthen active targeting.

Ni Dong1, Zhenyun Liu1, Haisheng He1

  • 1Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai 201203, China.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|January 14, 2023
PubMed
Summary
This summary is machine-generated.

Shape matters for nanoparticle drug delivery. Disk-shaped nanoparticles with folic acid-modified red blood cell membranes show enhanced targeting efficiency due to multivalent interactions, improving cancer treatment in mice.

Keywords:
Chronic myeloid leukemiaDoxorubicinDrug deliveryMultivalent interactionNanoparticleShapeTargeting

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Drug Delivery Systems

Background:

  • Enhancing active targeting efficiency of nanoparticles remains a significant challenge in drug delivery.
  • Multivalent interactions, involving multiple ligand-receptor bindings, are crucial for improving binding affinity.
  • The 'Hook&Loop' rationale suggests flat nanoparticle conformations may facilitate simultaneous multivalent binding.

Purpose of the Study:

  • To investigate the influence of nanoparticle shape on multivalent interactions and active targeting efficiency.
  • To synthesize and characterize spherical, rod-shaped, and disk-shaped folic acid-modified red blood cell membrane-coated biomimetic mesoporous silica nanoparticles (FRMSNs).
  • To evaluate the in vitro and in vivo performance of FRMSNs for enhanced active targeting.

Main Methods:

  • Preparation and physical characterization (morphology, shape, surface features) of FRMSNs with varying shapes.
  • In vitro studies involving K562 cells to assess binding and internalization of FRMSNs.
  • In vivo evaluation in K562 xenograft mice using doxorubicin-loaded disk-shaped FRMSNs to monitor therapeutic efficacy.

Main Results:

  • Disk-shaped FRMSNs exhibited strengthened binding and internalization by K562 cells compared to other shapes.
  • Bio-Transmission Electron Microscopy (Bio-TEM) visually confirmed 'plane' contact of disk-shaped particles with cells.
  • Quantification demonstrated enhanced binding affinity with folate binding proteins for disk-shaped FRMSNs due to multivalent interactions.
  • Doxorubicin-loaded disk-shaped FRMSNs effectively slowed the progression of chronic myeloid leukemia in K562 xenograft mice.

Conclusions:

  • Nanoparticle shape significantly impacts multivalent interactions and active targeting efficiency.
  • Disk-shaped nanoparticles favor multivalent interactions, leading to superior binding and cellular uptake.
  • The findings support the 'Hook&Loop' rationale and highlight the potential of disk-shaped FRMSNs for improved cancer therapy.