Background
Trehalose is a naturally occurring non-reducing disaccharide that is widely distributed in nature. It was first discovered in the ergosterol fungus of rye, and later was found in many organisms and microorganisms. For instance, in some organisms that survive in extreme environments, such as plants in deserts and insects in Antarctica, the content of trehalose in their bodies is relatively high. This is because trehalose has a strong ability to protect biological macromolecules from damage caused by environmental stress.
Structure and Characteristics
Trehalose is a non-reducing disaccharide, formed by the linkage of two glucose molecules through an α,α – 1,1 glycosidic bond. This unique structure endows it with numerous excellent properties. It has a high glass transition temperature (approximately 120℃), meaning that trehalose can maintain a stable glass state at higher temperatures and is not prone to crystallization. Additionally, trehalose has poor water absorption, a low crystallization rate, and does not contain reducing groups in its molecule, thus not undergoing oxidation-reduction chemical reactions with the active components in drugs. These characteristics give trehalose unique advantages in pharmaceutical applications, laying a solid foundation for its widespread use in various aspects.
High glass transition temperature
Stronger hydration ability
Not prone to form ice crystals
High temperature and humidity resistance, acid resistance
The application in medicines
01The “protector” for freeze-drying of biological products
In the field of biopharmaceuticals, such as vaccines, antibody drugs, and enzyme-based drugs, many active ingredients are extremely sensitive to environmental changes. Although freeze-drying technology can effectively extend their shelf life, the low temperatures and dehydration during the freeze-drying process may cause the biological active substances to denature and lose their activity. At this time, trehalose steps in as an ideal freeze-drying protective agent.
From the perspective of the mechanism of action, currently there are mainly the “water substitution hypothesis” and the “glass state hypothesis”. In simple terms, during the freeze-drying process, trehalose can form a protective layer on the surface of biological molecules, just like giving fragile biological molecules a sturdy armor. On one hand, it can replace water molecules to form hydrogen bonds with biological molecules, maintaining their natural conformation; on the other hand, the glassy structure formed by trehalose can inhibit the growth of ice crystals and reduce the physical damage caused by ice crystals to biological molecules.
02Microneedle formulation’s”Good assistant”
Trehalose can be used as a plasticizer or filler and added to the needle-making material of microneedles. It can regulate the hardness and flexibility of the microneedles, ensuring that they maintain sufficient strength to penetrate the skin while also having a certain degree of toughness, thereby reducing the risk of the microneedles breaking during use. Moreover, trehalose has good biocompatibility and generally does not cause an immune response in the body. The use of trehalose in microneedle preparations helps to reduce the immunogenicity of the entire preparation, minimize the potential immune-related adverse reactions caused by the use of microneedle preparations, and improve the safety and tolerance of the preparation.
03 Thickeners and stabilizers
In liquid preparations such as eye drops and oral liquids, trehalose plays a crucial role as a thickening agent and stabilizer. As a thickening agent, trehalose can increase the viscosity of the solution, allowing the drug to remain in the target area for a longer period and enhancing the bioavailability of the drug. In eye drops, a suitable viscosity of trehalose solution enables the drug to better adhere to the eye surface, prolonging the contact time between the drug and the ocular tissues, and enhancing the efficacy.
Meanwhile, trehalose can regulate the osmotic pressure of liquid preparations, making it similar to the physiological environment of the human body and reducing irritation to the mucous membranes. It can also inhibit the growth of microorganisms, exerting a certain degree of preservative effect, effectively prolonging the shelf life of liquid preparations and ensuring the stable quality of the drugs within the valid period.
04 Medical devices
Trehalose is widely used in the medical device field. In the aspect of cell cryopreservation solutions, trehalose can regulate the intracellular osmotic pressure, preventing cell swelling or shrinkage caused by osmotic pressure changes during freezing and thawing. It can replace water molecules to combine with biological macromolecules such as proteins and nucleic acids inside the cells, maintaining their natural structure and function, avoiding their denaturation due to dehydration, thereby maintaining the stability of the intracellular environment. In the storage of oocytes, trehalose can lower the freezing point of oocytes, reducing the possibility of ice crystal formation. In addition, it can form a glassy state inside the cells, keeping the substances inside in a stable amorphous state, avoiding damage caused by ice crystal growth and solute effect, thereby improving the tolerance of oocytes to freezing and facilitating their long-term storage and subsequent applications.
Advantages
Trehalose, as a natural sugar, has been recognized by multiple authoritative institutions such as the US Food and Drug Administration (FDA) and the European Food Safety Authority (EFSA) as a safe food additive and pharmaceutical excipient. In the pharmaceutical field, its safety has been widely verified. Japanese researcher Linrong strictly controls key indicators such as the purity, content, microbial limits, and endotoxin levels of trehalose.
Ultra-high purity (with a main content reaching 99.9%)
Ultra-low endotoxin (less than 0.6 EU/g)
CDE registration number: F20170000105 “A”
Compliant with USP/EP/JP/Ch
Stronger hydration ability
Higher glass transition temperature
Resistant to high temperature and humidity, acid resistance
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