Drug Delivery

Localized or targeted drug delivery systems have become the preferred choice for drug delivery, and their main goals are to minimize the adverse effects of drugs and address the unmet and emerging needs for better patient compliance^[1]. However, merely changing the drug formulation or molecule is not sufficient to maximize targeted therapy clinical efficacy. Click chemistry is a novel method for drug delivery in the diagnosis and treatment of diseases due to its high specificity, quick reaction rate, and stability, which greatly promote drug safety and effectiveness.

Applications

In cancer therapy, tumor tissue or cancer cell-specific drug delivery is highly needed to improve therapeutic efficacy and avoid adverse effects. Studies showed that copper-free click chemistry is a powerful tool for the labeling and targeting of cancer cells. Koo et al^[2]. carried out successful tumor-targeting drug delivery using bioorthogonal chemical receptors and the strain-promoted azide-alkyne cycloaddition (SPAAC) click reaction. They introduced azide groups into tumor cells in subcutaneous tumor-bearing mice by intratumorally injecting Ac4ManNAz. Then, DBCO conjugated PEGylated liposomes were intravenously injected into tumor-bearing mice and were bind on the target cancer cell surface by in vivo bioorthogonal SPAAC click reaction (Scheme 1). Here, DBCO acts as a drug carrier to deliver drugs to the cancer cell surface through the azide groups.

Scheme 1. Schematic illustration of in vivo tumor-targeting drug
delivery by bioorthogonal copper-free click chemistry.

In addition, click reaction plays an important role in the preparation and functionalization of polymeric and inorganic drug delivery carriers. For example, the use of C₆₀ for drug delivery was first demonstrated by Steinmetz and co-workers via the synthesis of derivatives of C₆₀ (buckyball) conjugated to virus NPs using CuAAC click reaction^[3].

What Can We Do?

Alfa Chemistry has a strong research foundation in the field of drug delivery. We have ability to help you explore the various applications of click chemistry and provide you with related click chemistry reagents, technical advice and services. If you have problems, please don't hesitate to contact us.

References

1. Meghani, N.M.; et al. Mechanistic applications of click chemistry for pharmaceutical drug discovery and drug delivery. Drug Discovery Today. 2017, 11(22): 1604-1619.
2. Koo, H.; et al. Bioorthogonal copper-free click chemistry in vivo for tumor-targeted delivery of nanoparticles. Angewandte Chemie. 2012, 47(124): 12006-12010.
3. Steinmetz, N.F.; et al. Buckyballs meet viral nanoparticles: candidates for biomedicine. Journal of the American Chemical Society. 2009, 47(131): 17093-17095.