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Updated: May 7, 2026

Nanomechanics of Drug-target Interactions and Antibacterial Resistance Detection
Published on: October 25, 2013
Multidrug resistance: Physiological principles and nanomedical solutions
Sijumon Kunjachan1, Błażej Rychlik2, Gert Storm3,4
1Department of Experimental Molecular Imaging, Helmholtz Institute for Biomedical Engineering, RWTH Aachen University, Pauwelsstrasse 30, 52074 Aachen, Germany.
Abstract:
Multidrug resistance (MDR) is a pathophysiological phenomenon employed by cancer cells which limits the prolonged and effective use of chemotherapeutic agents. MDR is primarily based on the over-expression of drug efflux pumps in the cellular membrane. Prominent examples of such efflux pumps, which belong to the ATP-binding cassette (ABC) superfamily of proteins, are Pgp (P-glycoprotein) and MRP (multidrug resistance-associated protein), nowadays officially known as ABCB1 and ABCC1. Over the years, several strategies have been evaluated to overcome MDR, based not only on the use of low-molecular-weight MDR modulators, but also on the implementation of 1-100(0) nm-sized drug delivery systems. In the present manuscript, after introducing the most important physiological principles of MDR, we summarize prototypic nanomedical strategies to overcome multidrug resistance, including the use of carrier materials with intrinsic anti-MDR properties, the use of nanomedicines to modify the mode of cellular uptake, and the co-formulation of chemotherapeutic drugs together with low- and high-molecular-weight MDR inhibitors within a single drug delivery system. While certain challenges still need to be overcome before such constructs and concepts can be widely applied in the clinic, the insights obtained and the progress made strongly suggest that nanomedicine formulations hold significant potential for improving the treatment of multidrug-resistant malignancies.
Insights
Multidrug resistance (MDR) in cancer limits chemotherapy effectiveness due to drug efflux pumps. Nanomedicine offers strategies to overcome MDR by using novel drug delivery systems and combination therapies.
Area of Science:
- Oncology
- Nanomedicine
- Pharmacology
Background:
- Multidrug resistance (MDR) in cancer cells impedes effective chemotherapy.
- Overexpression of ATP-binding cassette (ABC) transporters like P-glycoprotein (Pgp/ABCB1) and MRP (ABCC1) drives MDR.
- Current chemotherapeutic strategies face limitations due to MDR.
Purpose of the Study:
- To review nanomedical strategies for overcoming MDR in cancer.
- To discuss the physiological basis of MDR and its molecular mechanisms.
- To explore the potential of nanomedicine in treating multidrug-resistant malignancies.
Main Methods:
- Review of existing literature on MDR mechanisms and nanomedicine applications.
- Analysis of strategies involving carrier materials with anti-MDR properties.
- Evaluation of nanomedicines for altering cellular drug uptake.
- Assessment of co-formulation approaches combining drugs with MDR inhibitors.
Main Results:
- Nanomedicine offers diverse strategies to combat MDR, including intrinsic anti-MDR materials and modified cellular uptake.
- Co-formulation of chemotherapeutics with MDR inhibitors in nanodelivery systems shows promise.
- Nanomedical approaches can overcome limitations imposed by drug efflux pumps.
Conclusions:
- Nanomedicine formulations demonstrate significant potential for improving treatment outcomes in multidrug-resistant cancers.
- While clinical translation faces challenges, nanomedicine represents a promising frontier in oncology.
- Further research and development are crucial for widespread clinical application of these nanomedical strategies.
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