Drug Delivery Revolution: How Lipid Nanoparticles Are Changing the Game
- Evan Moloseni
- Jun 28
- 5 min read
The potential for lipid-based nanoparticle (LNPs) based pharmaceuticals has been increasingly recognised in recent years, especially in the medical research sector (Mehta et al., 2023). In other words, LNPs are a vital innovation into the already novel discovery of drug delivery using nanotechnology. But before we delve into the characteristics and mechanisms that make LNPs so great let's first get the basics out of the way.
Introduction to Lipid Nanoparticle delivery
A lipid shell surrounding an internal core composed of reverse micelles that encapsulate and deliver nucleic acids, like siRNA and mRNA, and plasmid DNA, ranging from 10 to1000 nanometers.(Intro to Lipid Nanoparticle Formulation, 2022).
As mentioned before, LNPs have been rising in popularity as they have built a market value of $3.5 billion in 2021compound annual growth rate of around 18.5% from 2021 to 2026 especially in fields such as oncology (Verma et al., 2023b). Like all innovative discoveries, LNPs require thorough creation techniques to ensure stability during storage, quality control and regulatory compliance.
They require such meticulous preparation due to their specific characteristic, such as but definitely not limited to:
Highly uniform ( meaning that they are quite stable ). Allowing for intergration in a multitude of organ systems.
Stable suspension of individual particles. Indeed, ensuring stability and efficacy when delivering medical substances.
Comprehensive characterization including Transimission Electron Microscopes (TEM), UV-Vis, (a technique used to measure amount of UV light absorbed by a substance) and Dynamic Lighting Scattering (DLS). Aiding in synthesis process and identification of lipid nanoparticles within organisms.
Wide particle size range, correlating to the range of substances that can be transported.
Various surface properties: coated, functionalized or conjugated with biomolecules.
Broad applications.
These come in many different forms such as:
Cationic LNPs:
As the name suggests these nanoparticles have a positive charge which helps them to bind to negatively charged cell surfaces.
Ionizable LNPs:
These have no charge at first but become positively charged in certain conditions, helping with delivery inside of cells.
Neutral LNPs:
These nanoparticles do not have a charge which make them less likely to cause negative effects.
Customized LNPs:
Designed with specific features to improve delivery or targeting certain cells.
LNPs can be further specialized into subgroups: liposomes, nano emulsions, solid lipid nanoparticles, nanostructured lipid carriers, lipid polymer hybrid nanoparticle.
Table: Showing the applications of different LNP subgroups, (Verma et al., 2023)
LNP subgroup | Active Substance | Diseases/Applications | Products |
Liposomes | Doxorubicin/daunorubicin and other anticancer agents, paclitaxel, amphotericin B, verteporfin | Cancer, visceral leishmaniasis, HAV viral vaccine, age-related macular degeneration | Doxil, Mepact Abraxane, Albecet, Epaxal Visudyne and more. |
Nanoemulsion | Etomidate, profol, heparinoid, ibuprofen,cyclosporin A, ritonavir and saquinavir | Anesthetics, pain relief, immunosuppressants, antiviral HIV-1 medicine in adults and children | Diprivan, topical delivery, Sandimmun Neoral, Norvir and Fortovase. |
Solid Lipid nanoparticles | Mitoxantrone, doxorubicin, oxiconazole | Hepatocarcinoma, tinea fungal infection and inflammation. | Phuronic gel and more ( usually used for clinical research). |
Nanostructured lipid carriers | Acitretin, self-amplifying RNA and all-trans retinoic acids | Psoriasis, keratinizartion disorders, and most notable COVID-19 | Spikevax, comirnaty and other vaccines treatments invovled in medical research. |
Lipid polymer hybrid nanoparticle | Docetaxel | Pancreatic cancer, lung cancer with KRAS mutations, prostate cancer | Currently being used in clinical trials. |
As shown in the data above LNPS have many applications to numerous fields around healthcare, however they are still in development, allowing room for further development and applications that may have not been discovered yet. As you can see from the images above many of the lipid nanoparticle subgroups contain similar features ( such as the phospholipid head on the outside of the particle). Though, their nuanced differences what makes each of the particle specialized for their individual function, though each subgroup is critical for the advancement of human health and medical research.
Advantages compared to others
Efficient cell entry - Lipid nanoparticles are designed to fuse with the cell surface membrane, thus they can easily penetrate into different cell types and transport necessary drugs.
Targetted delivery - It is easier to incooperate surface modifications on the surface lipid nanoparticles compared to other popular drug delivery systems.
Protection - Lipid carriers ( like most other nanomaterials) are effective in protecting fragile genetic materials such as mRNA and DNA.
Biocompatibility - Due to the abundant presence of lipids within the human body, lipid nanoparticle delivery is far more biocompatible compared to other nano-delivery systems that utilise foreign molecules ( such as silica or metals).
Potential risks/hazards
Cell Damage - Potential for triglyceride aggregation within cells due to their insoluability property.
Liver Stress - Certain LNPs may trigger oxidative stress in the liver, reducing antioxidant defenses and causing inflammation.
Inflammation - Cationic LNPs can cause inflammation/liver enzyme spikes or blood-clotting issues.
Potential for toxicity - Variable toxicity depending the formula use to create lipid nanoparticle formula.
Discussion
Lipid nanoparticle in drug delivery has clearly shown its versatility in a range of diseases and it multiple advantages compared to other forms of nanotechnology used in drug delivery. Though like most forms of drug delivery, there is a lot more research required for us to make a true synopsis of the potential of this form of drug delivery before we can actively integrate into modern medicine entirely.
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