Tetrazine-modified Biopolymer-based Drug Delivery Service

Tetrazine-modified Biopolymer-based Drug Delivery Service

Client Satisfaction with Tetrazine-modified Biopolymer-based Drug Delivery ls Our Pursuit

CD BioGlyco has achieved significant milestones in the domain of providing GlycoCLICK™-based Drug Delivery Service through our cutting-edge technology platform and pioneering mindset. Our professional tetrazine-modified Biopolymer-based Drug Delivery service has been widely recognized and praised within the pharmaceutical industry through years of continuous research and practice. The specific application of tetrazine-modified polymers in drug delivery systems is to achieve click release of drugs through the Diels-Alder reaction with tetrazine-trans-cyclooctene (TCO), a complementary reactant of tetrazine. The specific steps of our tetrazine-modified biopolymer-based drug delivery service are as follows:

  • First, we synthesize polymers containing tetrazine functional groups by chemical synthesis or modification of existing polymers. These methods include interatomic transfer radical polymerization, epoxy resin ring-opening reactions, etc. Next, we utilize bioconjugation techniques to achieve TCO-modified drug design. Subsequently, the drug molecules are reacted with small molecule coupling agents bearing active TCO groups to form a stable structure under appropriate conditions and to ensure that the structure does not react non-specifically under physiological conditions.
  • Subsequently, the tetrazine-modified polymer is mixed with the TCO-modified drug in a click reaction to covalently bind the drug to the polymer.
  • Finally, we trigger the click reaction to release the drug from the polymer by changing the temperature, and pH, or adding a specific triggering agent.

Fig.1 Flowchart of tetrazine-modified biopolymer-based drug delivery.Fig.1 Process of tetrazine-modified biopolymer-based drug delivery service. (CD BioGlyco)

Publication Data

Technology: Reversed-phase high-performance liquid chromatography (HPLC), electrophoresis, and autoradiography

Journal: Bioconjugate Chemistry

IF: 4.031

Published: 2020

Results: This article describes a new method, the TCO linkage method, for improving tumor uptake. The method improves tumor uptake by enhancing blood circulation. Specifically, the researchers explored which of the tetrazine or TCO moieties contributed more to increased circulation and uptake by changing the structure of the moiety. In their experiments, they designed a variety of tetrazine and TCO moieties with different structures and performed a detailed comparative analysis. The results showed that the radiotracer was able to maintain a relatively long in vivo circulation half-life in the presence of the DiPhTz moiety. This implies that the DiPhTz moiety plays a key role in enhancing tumor uptake. In addition, in evaluating the performance of the system in tumor uptake, the researchers applied it to different targeting ligands. They found that different targeting ligands combined with the tetrazine-TCO linkage significantly increased the uptake of the tracer by tumor cells.

Fig.2 Reactive prodrugs triggered by a click reaction between trans-cyclooctene and tetrazine.Fig.2 Prodrugs activated through the inverse electron demand Diels-Alder mechanism. (Wang, et al., 2020)

Applications

  • Binding drugs to tetrazine-modified biopolymers for the formation of stable linkages is applied to enhance drug accumulation in tumor tissues while minimizing toxicity toward normal tissues.
  • Tetrazine-modified biopolymers can be used to combine with imaging markers such as fluorescent dyes or radioisotopes for real-time monitoring of localization and release from drug delivery systems.
  • Tetrazine-modified biopolymer is applied to encapsulate or modify a drug to form a slow and controlled-release drug delivery system. Such systems can control the rate and duration of drug release, thereby modulating the therapeutic dose and providing a long-lasting drug effect.

Advantages

  • Tetrazine-modified biopolymers exhibit enhanced stability due to their robust linkages, resulting in an extended lifespan. This inherent stability enables the drug delivery system to maintain its efficacy within the body for a prolonged duration and effectively prolongs the half-life of drugs, thereby augmenting its therapeutic effectiveness.
  • Tetrazine-modified biopolymers are multi-functional, due to they can be combined with a variety of functional molecules or markers, such as fluorescent dyes, to realize multiple drug delivery systems.
  • Controlled drug release can be achieved by modulating the binding rate and stability of tetrazines to the corresponding reactive functional groups.

CD BioGlyco provides comprehensive tetrazine-modified biopolymer-based drug delivery service, catering to diverse pharmacological characteristics for both conventional and cutting-edge drugs in the field of life sciences. If you need more about the details, please feel free to contact us.

References

  1. Wang, M.; et al. Tetrazine-TCO ligation: a potentially simple approach to improve tumor uptake through enhanced blood circulation. Bioconjugate Chemistry. 2020, 31(7): 1795-1803.
  2. Kondengadan, S.M.; et al. Click chemistry and drug delivery: A bird ' s-eye view. Acta Pharmaceutica Sinica B. 2023, 13(5): 1990-2016.
For research use only. Not intended for any clinical use.
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