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LDL receptors and their role in targeted therapy for glioma: a review
Shreya Pawar1, Tejaswi Koneru2, Eva McCord3
1Use-inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory, Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA; Troy High School, Troy, MI 48098, USA.
Abstract:
Gliomas are highly lethal forms of cancers occurring in the brain. Delivering the drugs into the brain is a major challenge to the treatment of gliomas because of the highly selectively permeable blood-brain barrier (BBB). Tapping the potential of receptor-mediated drug delivery systems using targeted nanoparticles (NPs) is a sought-after step forward toward successful glioma treatment. Several receptors are the focus of research for application in drug delivery. Low-density lipoprotein receptors (LDLR) are abundantly expressed in both healthy brains and diseased brains with a disrupted BBB. In this review, we discuss the LDLR and the types of NPs that have been used to target the brain via this receptor.
Insights
Targeting brain gliomas is challenging due to the blood-brain barrier. This review explores using low-density lipoprotein receptors (LDLR) and nanoparticles (NPs) for effective glioma drug delivery.
Area of Science:
- Neuro-oncology
- Nanomedicine
- Pharmacology
Background:
- Gliomas are aggressive brain cancers with poor prognoses.
- The blood-brain barrier (BBB) severely restricts drug entry into the brain, hindering effective glioma treatment.
- Targeted drug delivery systems offer a promising strategy to overcome BBB limitations.
Purpose of the Study:
- To review the role of Low-Density Lipoprotein Receptors (LDLR) in brain drug delivery.
- To discuss nanoparticle (NP) strategies for targeting LDLR to treat gliomas.
- To highlight advancements in receptor-mediated drug delivery for brain cancers.
Main Methods:
- Literature review of studies investigating LDLR expression in brain tissue.
- Analysis of nanoparticle designs and their efficacy in crossing the BBB via LDLR.
- Synthesis of current research on targeted drug delivery systems for glioma.
Main Results:
- LDLR are expressed in both healthy and diseased brain tissue, making them a viable target.
- Various nanoparticles have been engineered to leverage LDLR for brain-specific drug delivery.
- Targeting LDLR with NPs shows potential for improved glioma treatment outcomes.
Conclusions:
- LDLR represent a promising target for overcoming the BBB in glioma therapy.
- Nanoparticle-based drug delivery systems targeting LDLR offer a potential breakthrough for brain cancer treatment.
- Further research into LDLR-mediated NP delivery is crucial for clinical translation.

