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Updated: Nov 15, 2025
Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
Published on: February 8, 2017
Antibody conjugated lipid nanoparticles as a targeted drug delivery system for hydrophobic pharmaceuticals
Martine K Notabi1, Eva C Arnspang1, Morten Ø Andersen1
1SDU Biotechnology, Department of Green Technology, Faculty of Engineering, University of Southern Denmark, Campusvej 55, Odense M DK-5230, Denmark.
Abstract:
Cancer remains a significant health issue worldwide. The most common group of chemotherapeutic agents are small-molecule drugs, which often are associated with toxic side-effects and non-specific delivery, leading to limited therapeutic effect. This paper describes the development of a targeted drug delivery system based on lipid nanoparticles for cancer therapy. The lipid nanoparticles consist of a lipid core conjugated to an albumin stealth coating and targeting antibodies through thiol chemistry synthesized utilizing a one-step method. Applying the developed method, lipid nanoparticles with diameters down to 87 nm, capable of encapsulating small molecule compounds were synthesized. Cellular uptake studies of the lipid nanoparticles loaded with the model drug Nile red demonstrated that stealth-coating reduced non-specific cell uptake by up to a 1000-fold compared to free drug. Moreover, antibody-conjugation led to a significant cellular retargeting. Finally, it was shown that the lipid nanoparticles undergo cellular uptake through the endocytic pathway. The lipid nanoparticles are simple to synthesize, stabile in serum and have the potential to be versatile targeted towards receptors selectively expressed by diseased cells using antibodies. Thus, the system may reduce the toxic side-effects of cancer drugs while improving their delivery to cancer cells, increasing the therapeutic effect.
Insights
Researchers developed targeted lipid nanoparticles for cancer therapy. This novel drug delivery system enhances cancer cell targeting and reduces side effects, improving treatment efficacy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Cancer chemotherapy often involves small-molecule drugs with significant toxic side effects and non-specific delivery.
- Limited therapeutic effects are observed due to poor drug targeting and systemic toxicity.
Purpose of the Study:
- To develop a targeted drug delivery system using lipid nanoparticles for enhanced cancer therapy.
- To improve the specificity and efficacy of small-molecule chemotherapeutic agents.
Main Methods:
- Synthesized lipid nanoparticles with an albumin stealth coating and targeting antibodies via one-step thiol chemistry.
- Characterized nanoparticle size and drug encapsulation efficiency.
- Performed cellular uptake studies using Nile red-loaded nanoparticles and assessed endocytic pathways.
Main Results:
- Developed lipid nanoparticles down to 87 nm in diameter, capable of encapsulating small molecules.
- Stealth coating reduced non-specific cell uptake by up to 1000-fold compared to free drug.
- Antibody conjugation achieved significant cellular retargeting, with uptake via the endocytic pathway.
Conclusions:
- The developed lipid nanoparticles are simple to synthesize, stable in serum, and versatile for targeting cancer cells.
- This targeted delivery system shows potential to reduce chemotherapy side effects and improve therapeutic outcomes.
