Targeted Drug Delivery Systems in Cancer Therapy

Targeted drug delivery systems in cancer therapy aim to concentrate therapeutic agents at tumour sites while sparing healthy tissues, thereby enhancing efficacy and minimising systemic toxicity. These systems encompass a broad range of carriers, including lipid-based vesicles, polymeric nanoparticles, dendrimers and antibody–drug conjugates. Passive targeting exploits the enhanced permeability and retention (EPR) effect of tumour vasculature, whereas active targeting employs surface ligands—such as antibodies, peptides or aptamers—to recognise tumour-associated receptors. Advances in stimuli-responsive materials allow controlled drug release in response to pH, enzymes or external triggers, refining spatial and temporal delivery. Integration of imaging agents has given rise to theranostic platforms that permit real-time monitoring of biodistribution and treatment response. Recent progress has addressed challenges of carrier stability, immune clearance and heterogeneous tumour microenvironments. By tailoring physicochemical properties and ligand density, researchers are moving towards precision oncology, personalised regimens and combination strategies that co-deliver chemotherapeutics, immunomodulators or gene therapy vectors. These innovations hold global significance, promising to improve outcomes in diverse cancer types and to accelerate translation to clinical practice.

Research from Nature Portfolio

In one seminal study, a pegylated liposomal formulation of galbanic acid was engineered with an integrin-targeting RGD peptide to overcome the poor solubility of the antiangiogenic agent. The resultant vesicles demonstrated enhanced endothelial uptake, elevated tumour accumulation in murine models and synergistic antiproliferative effects when co-administered with pegylated liposomal doxorubicin, yielding superior antitumour efficacy with reduced vascular toxicity. In a complementary approach, trastuzumab-grafted poly(amidoamine) dendrimers were synthesised for the selective delivery of docetaxel to HER2-positive breast cancer cells. These bioconjugates exhibited increased binding and internalisation in HER2-overexpressing cell lines, improved induction of apoptosis and an enhanced pharmacokinetic profile in vivo, thereby illustrating the potential of antibody-decorated dendrimers to refine specificity and lower off-target effects.

Targeted Drug Delivery Systems in Cancer Therapy publication trend

The graph below shows the total number of articles in targeted drug delivery systems in cancer therapy across all publications each year (not limited to Nature Index journals).

Technical terms

Liposome: A spherical vesicle composed of one or more phospholipid bilayers used to encapsulate and deliver drugs.

Dendrimer: A highly branched, tree-like polymeric nanostructure with modifiable surface groups for drug conjugation.

PEGylation: The attachment of polyethylene glycol chains to a molecule or surface to improve solubility and reduce immune recognition.

Antibody–drug conjugate (ADC): A targeted therapy in which a cytotoxic drug is chemically linked to an antibody directed against a tumour-specific antigen.

Enhanced permeability and retention (EPR) effect: The tendency for nanoparticles to accumulate in tumour tissue due to leaky vasculature and impaired lymphatic drainage.

RGD peptide: A tripeptide ligand (arginine-glycine-aspartic acid) that binds integrins overexpressed on tumour and endothelial cells.

References

1. Anti‐HER2 Immunoliposomes: Antitumor Efficacy Attributable to Targeted Delivery of Anthraquinone‐Fused Enediyne. Advanced Science (2024).
2. Applications of liposomes and lipid nanoparticles in cancer therapy: current advances and prospects. Experimental Hematology & Oncology (2025).
3. Anti‐HER2 Super Stealth Immunoliposomes for Targeted‐Chemotherapy. Advanced Healthcare Materials (2023).
4. Trastuzumab-grafted PAMAM dendrimers for the selective delivery of anticancer drugs to HER2-positive breast cancer. Scientific Reports (2016).
5. Liposomal formulation of Galbanic acid improved therapeutic efficacy of pegylated liposomal Doxorubicin in mouse colon carcinoma. Scientific Reports (2019).