The Huisgen 1,3-dipolar cycloaddition reaction of organic azides and alkynes has gained considerable attention in recent years due to the introduction in 2001 of Cu(1) catalysis by Tornoe and Meldal, leading to a major improvement in both rate and regioselectivity of the reaction, as realized independently by the Meldal and the Sharpless laboratories. The great success of the Cu(1) catalyzed reaction is rooted in the fact that it is a virtually quantitative, very robust, insensitive, general, and orthogonal ligation reaction, suitable for even biomolecular ligation and in vivo tagging or as a polymerization reaction for synthesis of long linear polymers. The triazole formed is essentially chemically inert to reactive conditions, e.g. oxidation, reduction, and hydrolysis, and has an intermediate polarity with a dipolar moment of ∼5 D. The basis for the unique properties and rate enhancement for triazole formation under Cu(1) catalysis should be found in the high ∆G of the reaction in combination with the low character of polarity of the dipole of the noncatalyzed thermal reaction, which leads to a considerable activation barrier. In order to understand the reaction in detail, it therefore seems important to spend a moment to consider the structural and mechanistic aspects of the catalysis. The reaction is quite insensitive to reaction conditions as long as Cu(1) is present and may be performed in an aqueous or organic environment both in solution and on solid support.

Cu-catalyzed azide-alkyne cycloaddition.

https://cyberleninka.org/article/n/933162.pdf

Hydrogels in drug delivery: progress and challenges

Poly(ethylene glycol) (PEG) is the most used polymer and also the gold standard for stealth polymers in the emerging field of polymer-based drug delivery. The properties that account for the overwhelming use of PEG in biomedical applications are outlined in this Review. The first approved PEGylated products have already been on the market for 20 years. A vast amount of clinical experience has since been gained with this polymer--not only benefits, but possible side effects and complications have also been found. The areas that might need consideration and more intensive and careful examination can be divided into the following categories: hypersensitivity, unexpected changes in pharmacokinetic behavior, toxic side products, and an antagonism arising from the easy degradation of the polymer under mechanical stress as a result of its ether structure and its non-biodegradability, as well as the resulting possible accumulation in the body. These possible side effects will be discussed in this Review and alternative polymers will be evaluated.

Poly(ethylene glycol) in Drug Delivery: Pros and Cons as Well as Potential Alternatives

Stimuli-reponsive polymers and their bioconjugates

Utilization of polymers as biomaterials has greatly impacted the advancement of modern medicine. Specifically, polymeric biomaterials that are biodegradable provide the significant advantage of being able to be broken down and removed after they have served their function. Applications are wide ranging with degradable polymers being used clinically as surgical sutures and implants. In order to fit functional demand, materials with desired physical, chemical, biological, biomechanical and degradation properties must be selected. Fortunately, a wide range of natural and synthetic degradable polymers has been investigated for biomedical applications with novel materials constantly being developed to meet new challenges. This review summarizes the most recent advances in the field over the past 4 years, specifically highlighting new and interesting discoveries in tissue engineering and drug delivery applications.

/pdf/biomedical-applications-of-biodegradable-polymers-2db9gcyzxw.pdf

Biomedical Applications of Biodegradable Polymers

Click chemistry refers to a group of reactions that are fast, simple to use, easy to purify, versatile, regiospecific, and give high product yields. While there are a number of reactions that fulfill the criteria, the Huisgen 1,3-dipolar cycloaddition of azides and terminal alkynes has emerged as the frontrunner. It has found applications in a wide variety of research areas, including materials sciences, polymer chemistry, and pharmaceutical sciences. In this manuscript, important aspects of the Huisgen cycloaddition will be reviewed, along with some of its many pharmaceutical applications. Bioconjugation, nanoparticle surface modification, and pharmaceutical-related polymer chemistry will all be covered. Limitations of the reaction will also be discussed.

/pdf/click-chemistry-a-powerful-tool-for-pharmaceutical-sciences-4sw7fe0ds6.pdf

Click Chemistry, A Powerful Tool for Pharmaceutical Sciences

Bone-targeting macromolecular therapeutics.

Background: Rheumatoid arthritis (RA) is a chronic, systemic, inflammatory disease that affects approximately 0.5 – 1% of adults worldwide and commonly results in joint destruction and significant impairment in the quality of life. RA is considered an autoimmune disease with unknown etiology. Many pathogenic pathways of RA have been revealed recently, which has led to development of various novel therapies. Objective: The current treatments for RA fall into four categories: non-steroidal anti-inflammatory drugs, glucocorticoids, non-biological, disease-modifying antirheumatic drugs (DMARDs) and biological DMARDs. In this review, we discuss some of the most recent development in antirheumatic therapies. Methods: Using SciFinder Scholar and PubMed as our main search tools, we evaluated various newly developed therapies for RA. In each drug category, emphases are placed on the mode of action, limitations and new drug candidates from the patent search. Those therapies that are well-established are reviewed on...

Dong Wang

Papers

Click Chemistry, A Powerful Tool for Pharmaceutical Sciences

Bone-targeting macromolecular therapeutics.

The Development of Novel Therapies for Rheumatoid Arthritis.

Synthesis and evaluation of water-soluble polymeric bone-targeted drug delivery systems

Development of macromolecular prodrug for rheumatoid arthritis.