Lipid nanoparticle (LNP) manufacturing systems must have high accuracy, precision, and consistency to meet GMP requirements. Ideally, they would provide a continuous process from formulation through fill/finish for end-to-end production in a single unit. This would eliminate the need for human intervention, reducing the risk of contamination.
Lipid nanoparticles are a promising drug delivery system that can increase the bioavailability of incorporated active ingredients, regulate drug release and intracellular permeation, and reduce side effects. However, these formulations are expensive and require careful monitoring of the entire process. The best way to do this is by using an online platform that provides real-time data from start to finish.
The lipids used to make these drug carriers are typically derived from animal fats, oils, or synthetic lipids. The ionizable lipids are coated with a surfactant to form the particle’s core. The drug substance is embedded inside this lipid matrix. The resulting spherical particles have a 50-1000 nm diameter and are stable at human body temperature.
Lipid-based delivery systems can be used to deliver a variety of therapeutic agents, including small-molecule drugs and vaccines. In addition, they can be used to produce RNA or DNA-based gene therapies, which have significant therapeutic potential. These nucleic acid-based drugs have been shown to treat various diseases by silencing pathological genes or expressing beneficial proteins.
Compared to other colloidal carrier systems, lipid nanoparticle companies offer many advantages for drug delivery, such as ease of manufacture and low toxicity. In addition, they can be formulated to target specific cell types and tissues and can easily overcome physiological barriers such as the blood-brain barrier.
Lipid nanoparticles can be used to encapsulate both lipophilic and hydrophilic drugs. They are highly stable and can withstand the physical challenges of drug delivery to the body. They can also be formulated for topical, oral, pulmonary, or parenteral delivery. They have proven to be a cost-effective way of enhancing the bioavailability of poorly soluble drugs.
In addition, they are easy to manufacture and can be produced at an industrial scale. This makes them a good choice for developing complex formulations with high complexity and safety requirements. Lipid nanoparticles can encapsulate complex peptides, protein drugs, and nucleic acid therapeutics. This is because the lipids can stabilize the nucleic acids and protect them from degradation in aqueous environments.
The resumption of medical facilities and new product launches have boosted the demand for lipid nanoparticles in medicine during the COVID-19 pandemic. This is a crucial driver for the growth of the global lipid nanoparticle market. For example, some saw an increase of around 9.5% in their revenues from the sales of these products in 2021. They also witnessed a surge in revenue generation from the sale of lipid nanoparticles.
Nevertheless, there is still a lack of evidence demonstrating that SLNs are superior to other drug formulation principles such as oil, macroemulsion (ME), and nanoemulsions (NE). This is mainly because many studies only compare the properties of a single aspect, e.g., the chemical stability of incorporated AI or skin penetration efficacy.
Targeted drug delivery
Lipid nanoparticles (LNPs) are tiny spheres made of lipid molecules that encapsulate therapeutic agents until they dock with cell membranes and release their contents. These systems have many medical applications, including gene therapy and RNA vaccines. However, they must be formulated with various factors to achieve their desired effects. These include drug loading efficiencies, stability, and minimum toxicity. They should be eliminated from the body after their function is complete. Several LNPs have been designed with biodegradable designs to facilitate this process. For example, the lipid-based LNPs MC3 and ALC-0315 have ester linkages in their lipid tail that the body can hydrolyze. This can speed up the elimination of the carrier and reduce toxicity.
Solid lipid nanoparticles (SLNs) are the most extensively studied LNPs for lipophilic drug delivery. These are synthesized through a high-pressure homogenization (HPH) method and can be produced at a laboratory scale. Their lipid internal structure improves their chemical stability and physical properties, making them an excellent choice for oral, transdermal, pulmonary, nasal, ocular, and rectal administration.
Another essential benefit of SLNs is their ability to deliver drugs based on protein or polypeptide structures. These are difficult to produce using other formulations, but SLNs can increase the stability of these drugs and ensure that they reach their target site. In addition, SLNs can also be used to deliver cytotoxic drugs that inhibit cancer cell growth by blocking the P-glycoprotein transporter system.
Reduced side effects
Lipid nanoparticles can increase the bioavailability of drugs, regulate their release and improve intracellular permeation. They also minimize the occurrence of treatment side effects and enable more precise drug delivery to targeted tissues. This is particularly important for poorly water-soluble compounds, such as the cancer drug paclitaxel. In contrast to the Chremophor El-based formulation, which produces significant side effects, patients tolerate Abraxane (a paclitaxel nanotherapeutic) well.
Lipids have a high degree of solubility and stability in water. Therefore, lipid nanoparticles can deliver drugs to the bloodstream and other sites in the body, such as the intestines, colon, and brain. This reduces the active ingredient’s toxicity and the drug required for effective treatment.
One of the most common methods for preparing lipid nanoparticles is high-pressure homogenization. This process involves forcing a mixture of lipids, water, and surfactant through small diameter tubes at very high pressures. This causes cavitation, resulting in the formation of a lipid nanoparticle dispersion. However, this energy-intensive method exposes the sample to temperature-stress conditions, which could cause undesirable interactions with heat-sensitive compounds.
Another method for preparing lipid nanoparticles uses a microemulsion technique. In this method, the lipid matrix with the drug is melted in an aqueous phase at temperatures above its melting point and then dispersed into an aqueous surfactant solution by high-speed stirring. The emulsion is then subjected to ultrasound irradiation, which reduces the size of the lipid particles and allows them to form microcapsules. This method requires less time than the high-pressure homogenization technique and can be used to prepare both SLNs and NLCs.