Click chemistry and drug delivery: A bird's-eye view

Click chemistry has been proven to be very useful in drug delivery. Due to the availability of a large number of click reactions with a various characteristics, selection of appropriate chemistry for a given application is often not a trivial task. This review is written for pharmaceutical researchers who are interested in click chemistry applications and yet may not be click chemistry experts. For this, the review gives an overview of available click reactions organized by application types. Further, the general under-standing of click reactions being fast and high yielding sometimes overshadows the need to analyze re-action kinetics in assessing suitability of a given reaction for certain applications. For this, we highlight the need to analyze the relationship among reaction kinetics, concentration effects, and reaction time scales, knowing that lack of such analysis could easily lead to failures. Further, possible issues such as chemical stability with various click reagents are also discussed to aid experimental designs. Recent ex-amples and extensive references are also provided to aid in-depth understanding of technical details. We hope this review will help those interested in using click chemistry in drug delivery to select the appro-priate reactions/reagents and minimize the number of pitfalls.(c) 2023 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

Automated summary

Click chemistry has proven to be useful in drug delivery, but selecting the appropriate chemistry is not easy. This review provides an overview of available click reactions for pharmaceutical researchers interested in click chemistry applications. It emphasizes the analysis of reaction kinetics, concentration effects, and reaction time scales to avoid failures. The review also discusses issues like chemical stability and provides recent examples and extensive references for a better understanding of technical details.