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Updated: Feb 17, 2026
Preparation of Neutrally-charged, pH-responsive Polymeric Nanoparticles for Cytosolic siRNA Delivery
Published on: May 2, 2019
Targeted Delivery of siRNA Therapeutics to Malignant Tumors
Qixin Leng1, Martin C Woodle2, A James Mixson1
1Department of Pathology, University of Maryland School of Medicine, 10 S. Pine St., Baltimore, MD 21201, USA.
Abstract:
Over the past 20 years, a diverse group of ligands targeting surface biomarkers or receptors has been identified with several investigated to target siRNA to tumors. Many approaches to developing tumor-homing peptides, RNA and DNA aptamers, and single-chain variable fragment antibodies by using phage display, in vitro evolution, and recombinant antibody methods could not have been imagined by researchers in the 1980s. Despite these many scientific advances, there is no reason to expect that the ligand field will not continue to evolve. From development of ligands based on novel or existing biomarkers to linking ligands to drugs and gene and antisense delivery systems, several fields have coalesced to facilitate ligand-directed siRNA therapeutics. In this review, we discuss the major categories of ligand-targeted siRNA therapeutics for tumors, as well as the different strategies to identify new ligands.
Insights
Ligand-targeted small interfering RNA (siRNA) therapeutics are advancing rapidly, utilizing novel ligands to deliver siRNA specifically to tumors. This review covers ligand categories and identification strategies for improved cancer treatment.
Area of Science:
- Biotechnology
- Molecular Biology
- Oncology
Background:
- Significant progress in identifying ligands for targeting tumor surface biomarkers over the past 20 years.
- Development of tumor-homing peptides, aptamers, and antibodies has been revolutionized by advanced techniques.
Purpose of the Study:
- To review major categories of ligand-targeted small interfering RNA (siRNA) therapeutics for tumors.
- To discuss diverse strategies for identifying novel ligands for therapeutic development.
Main Methods:
- Phage display
- In vitro evolution
- Recombinant antibody methods
Main Results:
- Identification of diverse ligands targeting tumor-specific biomarkers.
- Advancements in developing targeted delivery systems for siRNA therapeutics.
Conclusions:
- The field of ligand development for targeted therapeutics is continuously evolving.
- Integration of ligand-directed strategies holds promise for advanced siRNA therapeutics in oncology.
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