Reducing Environmental Pollution by Antibiotics through Design for Environmental Degradation

Abstract

The spread of antibiotic-resistant pathogenic bacteria is an increasing health issue worldwide. A possible origin of antibiotic resistance could be the persistence of antibiotics in the aquatic environment. To tackle this problem, restricted control of application of antibiotics in human and veterinary medicine has been proposed. However, these measures do not prevent the spread of antibiotic resistance but may delay the process, since antibiotics are still continuously emitted into the environment and many persist there. Derived from ciprofloxacin (CIP), CIP-Hemi, a fluoroquinolone with improved environmental properties, was developed following the benign by design approach and using in silico and in vitro methods. CIP-Hemi was designed to maintain its required metabolic stability (human liver microsomes, intestinal microsomes, blood plasma) and antibiotic activity (MIC in the μg mL −1 range) against the target while transforming into an inactive fragment (CIP-d-CP) and a degradable linker present under acidic conditions, e.g., after excretion or when released into the environment. Moreover, CIP-Hemi and CIP-d-CP showed weaker cytotoxic and mutagenic or genotoxic effects compared to the parent compound CIP and therefore underline the feasibility of CIP-Hemi as a viable antibiotic drug candidate, demonstrating benign by design as a promising approach.

Aptamer-functionalized fluorine-containing DNAsomes for targeted drug delivery to cancer cells

“…Similar mechanisms for the release of DOX have also been proposed in other vesicle systems and DNA-based nanostructures. 35–37 Our results undoubtedly demonstrate the potential of Sgc8/DOX/DNAsome for targeted drug delivery to cancer cells and further targeted cancer therapy.…”

GREENER Pharmaceuticals for More Sustainable Healthcare

“…Examples of APIs that are completely (bio)degradable in the environment are summarized elsewhere. 23 , 26 The desired properties for improved environmental degradation do not have to interfere with the API’s administration to patients. 23 To identify environmental (bio)degradability in the drug discovery process, medium-throughput screening assays are needed.…”

Molecularly Imprinting–Aptamer Techniques and Their Applications in Molecular Recognition

“…The adverse effects of antibiotics include allergic reactions and liver and kidney damage and can pollute the water environment. The use of antibiotics and the detection of residues in food has received considerable interest [ 59 , 60 , 61 ]. Materials that have dual recognition functions and are based on MIP–aptamer have been used in the recognition and analytical detection of antibiotics in real samples.…”