Today’s cyclodextrin is this great patent from Roquette‘s team, Tao Peng, Lucas Goh, Jeff Chang Shih Chieh on a new class of Lipid nanoparticles (LNPs) that can be used for nucleic acid delivery, wherein LNPs comprise a nucleic acid and a nonionic or cationic cyclodextrin compound.
How do you see the future of CDs in gene therapy? Will we see solutions commercialized in the future? In GENEGUT we certainly work towards this goal!
In this work and using kneading, we have compared the encapsulation of progesterone, a lipophilic hormone used in hormone replacement therapy, with β-CD and Nanosponges. The project opens the door to new medical formulations of progesterone, supporting the ball-milling kneading as an exciting way of making complexes.
Drug repositioning is a high-priority and feasible strategy in the field of oncology research, where the unmet medical needs are continuously unbalanced. Disulfiram is a potential non-chemotherapeutic, adjuvant anticancer agent. However, the clinical translation is limited by the drug‘s poor bioavailability. Therefore, the molecular encapsulation of disulfiram with cyclodextrins is evaluated to enhance the solubility and stability of the drug.
Throughout the different cancer cell lines‘ characteristics and disulfiram unspecific antitumoral activity, the inhibitory efficacy of the cyclodextrin encapsulated drug on melanoma (IC50 about 100 nM) and on glioblastoma (IC50 about 7000 nM) cell lines differ by a magnitude. This pre-formulation screening experiment serves as proof of concept for using cyclodextrin encapsulation as a platform tool for further drug delivery development in repositioning areas.
Today’s cyclodextrin is a small tribute to a huge contribution to the industrial cyclodextrin applications.
WACKER Chemical Corporation (WCC) established its Eddyville bioprocessing plant in 1999 and recently celebrated its 25th anniversary. The facility manufactures three different high-quality cyclodextrins: Alpha, Beta and Gamma. It is also the world’s sole commercial-scale manufacturer of Alpha and Gamma cyclodextrins.
Guided by WACKER’s global leadership, the Eddyville biotech facility has been at the forefront of cyclodextrin production since it was first built. The cyclodextrin products manufactured by WACKER became known worldwide under the trade names CAVASOL® and CAVAMAX®.
Last week between 10-14 June, the cream of cyclodextrin science gathered in Dunkerque, France to share their knowledge and most recent scientific results during the 21st International Cyclodextrin Symposium.
The conference started with a social tour, visiting nearby sights on the seashore and harbor and spending a wonderful lunch together. We concluded the first-day networking with a welcome party at the Town Hall.
During the event, we could enjoy 81 oral presentations spread across a 3 and half-day scientific fiesta. 166 participants from all around the world (75% Europe, 15% Asia, 10% America) exchanged ideas and initiated collaborations. The most well-represented countries were France, Italy, and Hungary (:P).
During the breaks, we could enjoy bites from French cuisine and discuss further science through the 56 presented posters.
Caitriona O’Driscoll from UCC giving her keynote
The 1st day was topped by a huge Dunkerque beer&cheese carnival, one of the most memorable social events of all time, while the 2nd one with a wonderful Gala dinner at the stunning nearby aquarium.
Bicyclos team at the Dunkerque Carnival
CarboHyde was represented by two members, Daniel Bisericaru and Tamas Sohajda, and presented a talk about the status, future and dilemmas of developing cyclodextrin-based active ingredients. Further collaborations of the company were dominated by sharing the results of two EU-funded projects: GENEGUT & Bicyclos HEurope.
Several awards were presented during the Symposium:
the prestigious Szejtli award went to Sophie Beeren for her groundbreaking work on novel enzymatic methods to create cyclodextrins
the best poster award to Ana Francisca Soares from Genegut on CD-based gene delivery
the best flash presentation to Martina Dragone discussing peptide-CD interactions
the best oral presentation to Clara Testard presenting high-level cyclodextrin synthesis
The conference was concluded by sharing future events where professionals can meet again:
Francesco Trotta will organize a CD Summer school in June, 2025 in Geneva, mainly for students
The next EUROCD will be held in Milano, September, 2025 as shown by Andrea Mele
Keiichi Motoyama invited attendees to Kyoto for the next Asian CD conference to be held in November, 2025.
Today’s cyclodextrin is a fascinating example of how to use the scavenging capabilities of cyclodextrins to develop tools against natural toxins by Alex Fragoso’s team.
Tetrodotoxins (TTXs) are potent marine neurotoxins involved in humans’ poisoning cases after consuming some marine organisms. In this work, five insoluble cyclodextrin polymers with different chemical structures have been investigated as novel clean-up materials for oyster extracts containing TTXs.
The best recoveries have been achieved with βCDP-14-DS2 (∼100 %), which allowed exposing cells to 27-fold higher oyster matrix concentrations and decreased the LOQ down to 46 µg equiv. TTX/kg.
Then, the applicability of this strategy has been demonstrated with oyster extracts from The Netherlands and comparing the results with immunoassay and liquid chromatography-tandem mass spectrometry (LC-MS/MS). This clean-up strategy combined with CBA could be implemented for TTXs detection in monitoring programs to ensure seafood safety.
Today’s cyclodextrin is about the stabilization effect of CDs on proteins, yet from a different angle.
I shared a lot earlier about the potential of CDs replacing surface active agents, yet how about combining them?
This study from Roquette led by Rajeev Gokhale and Vinod T. investigates the collaborative impact of combining polysorbates and HPβCD as excipients in protein formulations. The introduction of HPβCD in formulations showed it considerably reduced aggregation in two model proteins, bevacizumab and ipilimumab, following exposure to various stress conditions. The diffusion interaction parameter revealed a reduction in protein-protein interactions by HPβCD.
The study suggests that combining these excipients can improve mAb stability in formulations, offering an alternative for the biopharmaceutical industry.
Cluster Dextrin™, also called Highly Branched Cyclic Dextrin (HBCD) is a complex carbohydrate that is said to have several potential benefits for athletes and active individuals. It is manufactured from corn starch utilizing enzymatic reactions. Cluster dextrin provides a steady release of energy. Unlike the bonds in maltodextrin, which all break down at once, the bonds holding cluster dextrin together take more time to ‘unwrap’, and this results in your body being ‘drip fed’ with carbs.
Unfortunately, as seen below, it is also often referred to as cyclodextrin, which as we know is a different molecule, although it is also manufactured from corn starch utilizing enzymatic reactions, moreover, it is a complex carbohydrate that is said to have several potential benefits for athletes and active individuals.
Amorphous solid dispersions (ASDs) are frequently employed to improve the bioavailability of poorly soluble molecules by enhancing the rate and extent of dissolution in the drug product development process. These systems comprise an amorphous active pharmaceutical ingredient stabilized by a polymer matrix to provide enhanced stability.
Amorphous products, particularly ASDs, are currently the most emerging area in the pharmaceutical field. This strategic approach presents a huge impact and advantageous features concerning the overall improvement of drug product performance in clinical settings, which ultimately leads to drug product approval by leading regulatory agencies into the market.
Today’s cyclodextrin post sheds light on the fascinating ability of cyclodextrins to complex not only solids and oils, but also gases!
Researchers Todor Dudev and Tony Spassov from Sofia University explore the intimate mechanism of β-cyclodextrin/gas complex formation and answer intriguing questions.
They investigate how the polarity and size of the guest molecule influence complexation thermodynamics, and which encapsulation process by the host macrocycle is more advantageous. They also examine the major factors governing the formation of the complex between β-cyclodextrin and gaseous substances. The research emphasizes the special role that the cluster of water molecules inside the host’s internal cavity plays in the encapsulation process.
