November 03, 2023
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Both sucrose and trehalose are non-reducing disaccharides, so there is no need to worry about Browning reactions caused by reducing groups.
Compared with sucrose, trehalose has the following advantages:
1. Tolerance to acidic environment
Sucrose has been reported to hydrolyze in a weakly acidic environment, while trehalose can tolerate an acidic environment at pH 3.0.
2. Good hydrolysis stability
Although both are disaccharides, the free energy of trehalose glycosidic bond is much lower than that of sucrose, resulting in a significantly lower hydrolysis rate of trehalose than that of sucrose. This also explains the mechanism why hydrolysis of sucrose has been reported during freezing or drying, while trehalose has not.
3. Low hygroscopicity
Trehalose has lower hygroscopicity, which can improve the long-term stability of lyophilized preparations during storage.
4. High viscosity
Compared with other sugars, trehalose has more hydrogen bonds to bind water, and the ability to form hydrogen bonds is stronger, and it is easier to bind with water molecules. This makes the preparation of trehalose less easily hydrolyzed in the form of a low water content (such as the water content of freeze-dried powder is generally < 1%).
Step 5: Dosage
Trehalose is usually able to achieve protective effects at lower concentrations than sucrose. For the two GSK vaccines, Shingrix has a protein antigen/sucrose ratio of 50μg/20 mg, while Arexvy has a protein antigen/trehalose ratio of 120μg/14.7 mg.
6. High glass transition temperature
For freeze-dried preparations, the drying temperature at the second drying stage should not be higher than the glass transition temperature, otherwise collapse will occur. The glass transition temperature of trehalose is higher than that of sucrose. Therefore, choosing trehalose as a lyophilized protective agent can select a higher secondary drying temperature within the permissible range of the process, thereby improving the lyophilized efficiency and reducing the lyophilized cost.
Brief summary
Trehalose is a new type of sugar protection agent, which has excellent characteristics of protecting organisms, biofilms, proteins and so on. It has outstanding performance in anti-drying, anti-high temperature, anti-freezing and other aspects, so it has become one of the important protective agents in new vaccines, antibody drugs, nucleic acid drugs, cell and gene treatment agents, living body cell freezing and other preparations. In the field of antibody coupling drugs, trehalose is widely used and is more common than traditional monoclonal drugs.
Avitron is a long-term supplier of injectable grade trehalose, sucrose, TRIS/ TRIS-HCL, HEPES and other bioprotectants and buffer salts. We are produced under GMP conditions, in line with the international mainstream pharmacopoeia standards, product quality has Chinese and American double report, and low internal toxin, in line with DNase& RNase free requirements. We are committed to assisting the research and development, production and application of biological agents such as recombinant protein vaccines, mRNA vaccines, adenovirus vector vaccines, liposomes, single and double antibodies, antibody coupling drugs.
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