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Date of publication:2021/4/26 9:36:00

Application of Lipid Nanoparticles in 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.

Category Pfizer-BioNTech mRNA vaccine Moderna mRNA vaccine
Product Name  BNT162b2/Tozinameran/Comirnaty mRNA-1273
mRNA dose 30 µg 100 µg
Route of administration intramuscular intramuscular
Lipid nanoparticle components ALC-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
Buffer Potassium dihydrogen phosphate
Disodium hydrogen phosphate dihydrate
Tris (tromethamine)
Other excipients Potassium 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. 

Category Product Name CAS NO. Link
PEG mPEG-N,N-Ditetradecylacetamide, ALC-0159  1849616-42-7 View Detailes>
mPEG2000-DMG
Polyethylene glycol [PEG] 2000 dimyristoyl glycerol [DMG]
160743-62-4 View Detailes>
mPEG2000-OH
Methoxypoly(ethylene glycol) 2000
9004-74-4 View Detailes>
mPEG-CH2CH2CH2-NH2
Methoxypoly (ethylene glycol) propylamine
—— View Detailes>
mPEG2000-CM
Methoxypoly(ethylene glycol) carboxymethyl 2000
—— View Detailes>
mPEG2000-DSPE 147867-65-0 View Detailes>
mPEG2000-DPPE 205494-72-0 View Detailes>
PC DSPC 816-94-4  View Detailes>
DPPC 63-89-8 View Detailes>
HSPC 92128-87-5 View Detailes>
DEPC 51779-95-4     View Detailes>
DOPC 4235-95-4    View Detailes>
DMPC 18194-24-6 View Detailes>
PG DPPG 200880-41-7   View Detailes>
DSPG 124011-52-5   View Detailes>
PE DSPE 1069-79-0  View Detailes>
DPPE 923-61-5 View Detailes>
DOPE 4004-05-1 View Detailes>
DMPE 998-07-2 View Detailes>
PA DPPA 71065-87-7 View Detailes>
DSPA 108321-18-2 View Detailes>

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