Nanotechnology in Cancer Therapy: A Concise Review of Active Targeting of Drug Delivery Systems

Introduction

A significant issue and one of the biggest challenges in cancer treatment today is the selective delivery to cancerous cells on one side, and sparing normal tissue on the other. Although conventional chemotherapy has proven to kill cancer cells, toxic effects are usually associated with it; poor bioavailability occurs as well as the development of drug resistance. Nanotechnology has developed as an enabling technology to overcome these challenges by providing the development of nanoparticle-based delivery systems (NDDS) that can be designed to have better pharmacokinetics, tumor accumulation, and selectivity ([2401.11192], 2024; Montoto, Muraca, & Ruiz, n.d.). Herein is a concentrated discussion of the prospect of active targeting in nanomedicine as an entire therapy of cancer, practically considering limitations and prospects.

Possibilities of Nanoparticle-Based Delivery Systems

NPs have unique physicochemical properties like nanoscale size, high surface area-to-volume ratio, and the ability to alter the surface chemistry that makes them an attractive delivery agent of cancer drugs (Montoto, Muraca, & Ruiz, n.d.). The Eurofins NDDS benefits are as follows:

• Long Lived and Prolonged Ability

  • Nanoparticles have the ability to be developed with stealth characteristics (e.g., PEGylation) to not be cleared rapidly by the mononuclear phagocyte system. It extends circulation time and leads to more likelihood of drug concentrating on the tumor sites ([2401.11192], 2024).

• Increase in ascent of hydrophobic drugs

  • The use of many potent anticancer agents is limited by their low water solubility, e.g., paclitaxel and doxorubicin. Formulation of the drug in liposomes, micelles or polymeric nanoparticles will increase solubility and maximize drug bioavailability  (Montoto, Muraca, & Ruiz, n.d.)..

• Regulated and Stimuli-Controlling Release

  • NanoDDS can be developed to achieve controlled drug release either by passive means (through degradation or diffusion), or in response to tumor microenvironmental cues, including acidic pH, elevated temperature, redox gradients, etc. This makes the drug release favorable at the site of the tumor without much systemic toxicity ([2401.11192], 2024).

Mechanisms of Targeted Delivery

Nanoparticles have potential in the delivery of therapeutics by two complementary routes:

• Passive Targeting (EPR Effect)

  • The leaky vasculature and lymphatic drainage in tumors tends to trap nanoparticles locally, in the tumor microenvironment to which they preferentially accumulate (Montoto, Muraca, & Ruiz, n.d.). This phenomenon of increased permeability and retention (EPR) is the basis of many of the first-generation nanomedicines, e.g. Doxil (liposomal doxorubicin). Nevertheless, interpatient and intrapatient variability of the EPR effect imposes a constraint on universal usefulness.

• Active Targeting

  • A further way to increase specificity is to functionalize nanoparticles with ligands that will bind to receptors overexpressed in tumor cells (e.g., monoclonal antibodies, aptamers, peptides, small molecules; receptors: folate receptor (liver/prostate/colorectal), HER2 (breast/ovarian), transferrin receptor (liver)). This ligand-receptor binding facilitates the activation of the receptor-dependent endocytosis increasing intracellular drug levels and also minimizing off-target effects ([2401.11192], 2024). Active targeting is a game changer to precision medication and it can be used in both going against both solid and hematological malignancies.

Nanoparticles as a Platform in Cancer Treatment

A variety of nanomaterial classes that have been studied with regard to therapeutic delivery exist, each having their own advantages:

• Polymeric Nanoparticles

  • Biodegradable materials can be used, for example, polylactic glycolic acid (PLGA) and polyethylene glycine (PEGylated structures) offer sustained release and can be made target specific (Montoto, Muraca, & Ruiz, n.d.). Their ease of conformation adapts them to hydrophilic and hydrophobic drugs.

• Liposomes

  • Liposomes are biomaterial bilayer lipid vesicles, which can be used to enclose an array of different drugs. Clinically licensed preparations (e.g., Doxil, DaunoXome) demonstrate the safety and the ability to minimize systemic Intoxication ([2401.11192], 2024).

• Dendrimers

  • Dendrimers are highly functionalized nano sized branched polymers. They have architecture enabling high drug loading and release control, as well as conjugation to targeting ligands (Montoto, Muraca, & Ruiz, n.d.).

• Inorganic Nanoparticles

  • Gold, silica, iron oxide and quantum dot nanoparticles may be formulated to serve simultaneous therapeutic and diagnostic applications (theranostics). As another example, gold nanoparticles are proposed in photothermal therapy where the heating effect of light destroys cancer tissue ([2401.11192], 2024).

Nanotechnology in Drug Resistance Over-coming Drug Resistance Nanotechnology in Drug Resistance

Multidrug resistance (MDR) due to mechanisms including efflux pumps (e.g. P-glycoprotein) and gene mutations, is a significant cause of failure of chemotherapy treatment (Montoto, Muraca, & Ruiz, n.d.). There are numerous methods, which may be used to overcome resistance suggested by nanotechnology:

• Bypass of Efflux Pump Nano-particles bypass efflux mechanisms because they allow the high local concentrations to be released intracellularly.

• Gene Silencing: Resistance related genes can be downregulated by delivery of siRNA or miRNA using nanoparticles.

• Combination Therapy: There may be a synergistic effect with the co-delivery of chemotherapy agents with efflux pump inhibitors or pathway-targeted drugs incorporated into the same nanoparticle.

Clinical Uses and Future Directions

Many NDDS have progressed into clinical trials with several currently approved to treat cancer. ([2401.11192], 2024). Examples include:

• Doxorubicin like GE Leukeran is given as liposomal doxorubicin under the brand name Doxil.

• Abraxane (paclitaxel-binding albumin)

• liposomal irinotecan (Onivyde)

Although these achievements are impressive, a number of issues still exist:

• Scalability and Manufacturing: Nanoparticle reproduction and large-scale manufacture is a difficult task to make sure quality and safety remain intact.

• Regulatory Hurdles: The standard guidelines to approve nanomedicine have not been set yet, and they will impede the translation of nanomedicine into clinical practice.

• Patient Variability: There is an inter-patient variability that harms the predictability of therapeutic efficacy due to variation in tumor biology, microenvironment, and EPR effect.

The prospective future nanomedicine promises to incorporate personalized medicine methods- with nanoparticle constructs personalized to a tumor profile of an individual. Moreover, convergence of nanotechnology with immunotherapy, gene editing (CRISPR-Cas9) and real-time imaging, hold the promise to create a new era of precision medicine(Montoto, Muraca, & Ruiz, n.d.).

Conclusion

Nanotechnology has transformed the new horizon of cancer therapy through the specific, controlled, and personalized treatment delivery of the drugs. NDDS have few unparalleled potentials in enhancing therapeutic potential of an anticancer agent, reducing the side effects and combating chemotherapy resistance. Although manufacturing, regulatory, and biological challenges still exist with regards to clinical translation, the future trends of nanomedicine suggest a time when site-specific and patient-tailored cancer therapy will be the new standard of care. Nanotechnology will be significant in oncology therapeutics of the next generation as the current research opens up a gap between laboratory advances and clinical applications ([2401.11192], 2024; Montoto, Muraca, & Ruiz, n.d.).

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Works Cited

[2401.11192] Smart Drug-Delivery Systems for Cancer Nanotherapy. (2024, January 20). arXiv. Retrieved August 19, 2025, from https://arxiv.org/abs/2401.11192

Montoto, S. S., Muraca, G., & Ruiz, M. E. (n.d.). Nanoparticle-Based Drug Delivery in Cancer Therapy and Its Role in Overcoming Drug Resistance. Frontiers. Retrieved August 19, 2025, from https://www.frontiersin.org/journals/molecular-biosciences/articles/10.3389/fmolb.2020.00193/full

Montoto, S. S., Muraca, G., & Ruiz, M. E. (n.d.). Nanoparticle-Based Drug Delivery in Cancer Therapy and Its Role in Overcoming Drug Resistance. Frontiers. Retrieved August 19, 2025, from https://www.frontiersin.org/journals/molecular-biosciences/articles/10.3389/fmolb.2020.00193/full

Image Citation

OpenAI. (2025). Nanoparticles targeting a cancer cell [AI-generated image]. ChatGPT (GPT-5). https://chat.openai.com/