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Application of Lipid Nanoparticles in COVID-19 mRNA Vaccines

Release time:2021/4/26 15:48:52
Author:Huateng

The use of lipid nanoparticles (LNPs) in BioNTech/Pfizer and Moderna COVID-19 mRNA vaccines.

Of all approved COVID-19 vaccines in the market, the vaccines developed by BioNTech/Pfizer and Moderna has received widespread attention from all over the world, which represent a new class of vaccine products: they are composed of messenger ribonucleic acid (mRNA) strands encapsulated in lipid nanoparticles (LNPs).

mRNA vaccines are new types of vaccines that have aroused great interest. The main challenge for their applications is how to ensure their effective delivery. This is because the physicochemical properties of mRNA (such as negative charge and hydrophilicity) hinder the passive diffusion of mRNA vaccines through the plasma membrane. Moreover, mRNA vaccines are also susceptible to nuclease degradation. For example, free mRNA will quickly decompose in the body, greatly reducing its effectiveness.

It is necessary to use advanced technology to avoid this situation, thereby improving the stability of the vaccine, and this is where the lipid nanoparticles(LNPs) come into play. Currently, the approved mRNA COVID-19 vaccines (Table 1) are utilizing LNP technology. This illustrates the successes achieved with this type of nanoparticle to stabilize mRNA and successfully deliver it into cells. To be specific, LNPs have two advantages as an mRNA vaccine vector. On the one hand, LNPs defend mRNA from degradation by enzymes from the endosome. The characteristic guarantees high encapsulation efficiency. On the other hand, LNPs have good biocompatibility through a series of biological processes to deliver mRNAs for expression.

CategoryPfizer-BioNTech mRNA vaccineModerna mRNA vaccine
Product Name BNT162b2/Tozinameran/ComirnatymRNA-1273
mRNA dose30 µg100 µg
Route of administrationintramuscularintramuscular
Lipid nanoparticle componentsALC-0315 = (4-hydroxybutyl) azanediyl)bis (hexane-6,1-diyl)bis(2-hexyldecanoate)
ALC-0159 = 2-[(polyethylene glycol)-2000]-N,N ditetradecylacetamide
1,2-Distearoyl-sn-glycero-3-phosphocholine (DSPC)
Cholesterol
SM-102=(heptadecan-9-yl 8-((2-hydroxyethyl) (6-oxo-6-(undecyloxy) hexyl) amino) octanoate}
PEG2000-DMG = 1-monomethoxypolyethyleneglycol-2,3-dimyristylglycerol with polyethylene glycol (2000)
1,2-Distearoyl-sn-glycero-3 phosphocholine (DSPC)
Cholesterol
BufferPotassium dihydrogen phosphate
Disodium hydrogen phosphate dihydrate
Tris (tromethamine)
Other excipientsPotassium chloride
Sodium chloride
Sucrose
Water for injection
Sodium acetate
Sucrose
Water for injection

Table 1:Approved mRNA COVID-19 vaccines

The LNPs in mRNA COVID-19 vaccines consist of four main components: a neutral phospholipid, cholesterol, a polyethylene-glycol (PEG)-lipid, and an ionizable cationic lipid, among them, PEG can enhance the stability and lifespan of LNPs. According to public information, PEG has never appeared in any other vaccines in the world. This will be another new application of PEG in the field of medicine.

Lipid Nanoparticles

The structure of lipid nanoparticle vaccine carrier: mRNA organized in reverse lipid micelles in the nanoparticles (A); mRNA embedded between lipid bilayers (B)

Huateng Pharma is a dynamic science company dedicated to PEG derivatives and intermediates. We are capable of supplying small to large quantities of a rich selection of PEG derivatives and fine chemicals to serve bio-technology and pharmaceutical companies and research organizations worldwide. We can supply the following products used in COVID-19 vaccines. 

CategoryProduct NameCAS NO.Link
PEGmPEG-N,N-Ditetradecylacetamide, ALC-0159 1849616-42-7View Detailes>
mPEG2000-DMG
Polyethylene glycol [PEG] 2000 dimyristoyl glycerol [DMG]
160743-62-4View Detailes>
mPEG2000-OH
Methoxypoly(ethylene glycol) 2000
9004-74-4View Detailes>
mPEG-CH2CH2CH2-NH2
Methoxypoly (ethylene glycol) propylamine
——View Detailes>
mPEG2000-CM
Methoxypoly(ethylene glycol) carboxymethyl 2000
——View Detailes>
mPEG2000-DSPE147867-65-0View Detailes>
mPEG2000-DPPE205494-72-0View Detailes>
PCDSPC816-94-4 View Detailes>
DPPC63-89-8View Detailes>
HSPC92128-87-5View Detailes>
DEPC51779-95-4    View Detailes>
DOPC4235-95-4   View Detailes>
DMPC18194-24-6View Detailes>
PGDPPG200880-41-7  View Detailes>
DSPG124011-52-5  View Detailes>
PEDSPE1069-79-0 View Detailes>
DPPE923-61-5View Detailes>
DOPE4004-05-1View Detailes>
DMPE998-07-2View Detailes>
PADPPA71065-87-7View Detailes>
DSPA108321-18-2View Detailes>