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Published on: February 19, 2016
Endogenous stimuli-responsive linkers in nanoliposomal systems for cancer drug targeting
Mahdi Faal Maleki1, Arash Jafari2, Elaheh Mirhadi3
1Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Abstract:
There are various drug delivery systems (DDSs) among which nanoliposomal formulations are among the most prominent. Despite the superiority of nanoliposomal DDSs compared to conventional drug delivery methods, recent reports have claimed that they can deliver small amounts of the injected dose to target site by passive targeting. However, our understanding of tumor microenvironment features, including dysregulation of pH, the high intracellular concentration of glutathione, change in the amount and expression of some enzymes, reactive oxygen species, hypoxia, and ATP concentrations, has driven the scope of research into the use of these endogenous stimuli for a design of smart linkers. These linkers optimize the release of payloads in favorable target sites and avoid premature releasing in non-favorable off-target sites. In this review, we discuss particular linkers, which are able to respond to the specific endogenous conditions, and could be used in nanoliposomal DDSs, based on pathophysiological changes that occur in tumors. Furthermore, structural and chemical properties of these linkers and other potential linkers, which could be used in nanoliposomal DDSs, have been reviewed.
Insights
Nanoliposomal drug delivery systems can be improved using smart linkers that respond to tumor microenvironment conditions. These linkers optimize drug release at the target site, enhancing therapeutic efficacy.
Area of Science:
- Biomedical Engineering
- Materials Science
- Drug Delivery Systems
Background:
- Nanoliposomal drug delivery systems (DDSs) are advanced compared to conventional methods.
- Passive targeting of nanoliposomal DDSs to tumors has shown limitations in delivering therapeutic payloads.
- Tumor microenvironment (TME) features like altered pH, glutathione levels, enzyme activity, reactive oxygen species, hypoxia, and ATP concentrations present unique opportunities for targeted drug release.
Purpose of the Study:
- To review endogenous stimuli-responsive linkers for nanoliposomal DDSs.
- To discuss linkers that leverage specific TME pathophysiological changes for targeted payload release.
- To explore structural and chemical properties of existing and potential linkers for nanoliposomal DDSs.
Main Methods:
- Literature review of nanoliposomal drug delivery systems.
- Analysis of tumor microenvironment characteristics.
- Evaluation of smart linker strategies for controlled drug release.
Main Results:
- Smart linkers can be designed to respond to specific TME stimuli, enabling targeted drug release.
- These linkers can prevent premature drug release in non-target sites, improving safety and efficacy.
- Various endogenous stimuli within the TME can be exploited for linker activation.
Conclusions:
- Responsive linkers are crucial for optimizing nanoliposomal DDS performance in tumor therapy.
- Understanding TME provides a basis for designing sophisticated, stimuli-responsive nanoliposomal DDS.
- Further research into linker chemistry and properties will enhance nanoliposomal DDS capabilities.
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