Cyclodextrin-enabled nepafenac eye drops with improved absorption open a new therapeutic window

drug delivery, ,

This research is close to my heart as it comes from a Hungarian collaboration on developing nepafenac eyedrops with improved absorption. The results showed that one formulation possessed better bioavailability ex vivo than Nevanac® 0.1 % suspension, while the other formulation containing only 60 % of the original dose was ex vivo equivalent with Nevanac® opening the way to nepafenac-containing eye drops with better patient compliance in the future.

Anna Vincze, Facskó Réka, Budai-Szűcs Mária, Gábor Katona, Benjámin Gyarmati, Anita Csorba, Dr. Zelkó Romána, Zoltán Zsolt Nagy, Lajos Szente, György Tibor Balogh,

See the full article here.

Discovery of natural-product-derived sequanamycins as potent oral anti-tuberculosis agents

carbohydrates, drug discovery

Amazing research on the drug discovery of a series of macrolides called sequanamycins (bacterial ribosome inhibitors) with outstanding in vitro and in vivo activity against Mycobacterium tuberculosis (Mtb). The mechanism of action is similar to that of erythromycin and clarithromycin, but with binding characteristics that allow them to overcome the inherent macrolide resistance of Mtb. SEQ-9 was efficacious in mouse models of acute and chronic TB as a single agent, and it demonstrated bactericidal activity in a murine TB infection model in combination with other TB drugs. These results support further investigation of this series as TB clinical candidates, with potential use in new regimens against drug-susceptible and drug-resistant TB.
Sanofi, Texas A&M University, Evotec – Jidong ZHANG, Kwame Amaning, Zhicheng (Z.Chen) Cui, Scott Franzblau, Florence Bordon-Pallier, Cathy Cantalloube, Stefaan Sansen, Laurent Fraisse, Alexey Rak, Lasse Jenner, Gulnara YUSUPOVA, Junjie Zhang, Takushi Kaneko, Nader Fotouhi, Sandeep Tyagi, Fabrice B., Anna Upton, James Sacchettini and Sophie LAGRANGE, PhD

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Formulation, composition or foodstuff additives for the modification of glycemic response methods of manufacturing and using the same 

Today's cyclodextrin,

The story of two stone and one bird:
It is very rare that different cyclodextrins are combined in the same formulation, but there are examples on the market. Hoow Foods‘s invention uses one CD which hides the unpleasant taste of any phenylpropanoid from the sensory receptors. This will have the added advantage that the phenylpropanoids will be protected from the acidic environment of the stomach allowing more of them to reach the intestines. Adding a second cyclodextrin that has not been complexed makes the composition behave similarly to known sugars and starches thereby minimising any effect on the texture of the foods to which it is added.

See the full patent on Espacenet

Increasing space-time-yield, carbon-conversion-efficiency and carbon substrate flexibility in the production of fine chemicals

carbohydrates, ,

Fascinating discovery from BASF on increasing space-time-yield, carbon-conversion-efficiency, and carbon substrate flexibility in the production of fine chemicals. They found a positive effect of increased cAMP levels and/or manipulating the PTS system on the above characteristics achieved by de-regulating adenylate cyclase cyaa by deleting the C-terminal regulatory region leading to increased cAMP levels or deleting the Crr protein activity (carbohydrate repression resistance) which regulates the carbohydrate utilization system. Both lead to increased 2-fucosyllactoe and 6-sialyllactose production (human milk oligosaccharides) and increase carbohydrate usage.
Hartwig Schroeder; Peter Ödman]; Georg Wandrey; Christian Dietzsch; Dominik Satory; Matthew Blankschien; Jens Plassmeier et al.

See the full patent on Espacenet

Preparation method of edible cell culture meat 3D scaffold using ionic crosslinking

carbohydrates,

Interesting invention about the preparation method of an edible cell culture meat 3D scaffold using ionic crosslinking of chitosan oligosaccharide and sodium alginate. The cell culture meat 3D scaffold prepared by the method does not use any animal source component, is safe and edible, has good cell adhesion and compatibility, is used for the culture of skeletal muscle cells, and provides support for the manufacturing of cell culture meat.

See the full patent on Espacenet.

Environment Modulates Protein Heterogeneity Through Transcriptional and Translational Stop Codon Miscoding

carbohydrates,

Cool research published by our scientific advisory board member Agnes Toth-Petroczy and her team about how the environment influences the accuracy of protein production, which increases protein heterogeneity when the organisms need to adapt to new conditions.
Maria Luisa Romero Romero, Jonas Pöhls, Tobias Jumel

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Dimethyl-α-cyclodextrin induces capacitation by removing phospholipids from the plasma membrane of mouse sperm 

Today's cyclodextrin

This is a sometimes forgotten application in the biotechnology field: fertilization. Capacitation is an important event in the completion of fertilization by mammalian sperm. cholesterol efflux is a trigger of capacitation. In general, cholesterol acceptors of albumin and β-cyclodextrins are used to induce capacitation during in vitro fertilization. Kumamoto University, JAPAN published a study using dimethyl-α-cyclodextrin (DMACD) that induced sperm capacitation and promoted fertilization ability better than other CDs before, highlighting the role of not only cholesterol but also other phospholipids in the process. These findings suggest that phospholipid efflux is a novel trigger of capacitation. Increasing the choice of sperm capacitation inducers may be useful for improving in-vitro fertilization (IVF) techniques in mice and various species in which it has been difficult to produce embryos by IVF.

See the full article here.

Hallmarks of neurodegenerative diseases

carbohydrates

An important review of the hallmarks of neurodegenerative diseases for like-minded researchers who deal with this challenging field. The framework can serve as a basis for defining pathogenic mechanisms, categorizing different NDDs based on their primary hallmarks, stratifying patients within a specific NDD, and designing multi-targeted, personalized medicine to halt NDDs effectively.
Thank you for this excellent compilation!
Hasselt University/National Institute Of Aging/KU Leuven/Washington University in St. Louis/University of Gothenburg – David M Wilson III, Mark Cookson, Ludo Van Den Bosch, Henrik Zetterberg, David Holtzman, Ilse Dewachter 

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Evaluation of polyanionic cyclodextrins as high affinity binding scaffolds for fentanyl

Today's cyclodextrin,

Fascinating application shared by Lawrence Livermore National Laboratory – Edmond Lau et al. on the synthesis of new CDs possessing extended thioalkylcarboxyl or thioalkylhydroxyl moieties and assess their binding affinity towards fentanyl hydrochloride. The performance of these host molecules portends their utility as platforms for medical countermeasures for opioid exposure, as biosensors, and in other forensic science applications.

See the full article on nature.com.