Study of progesterone complexation in cyclodextrins and cyclodextrin-based nanosponges as an example of solvent-free complexation

Today’s cyclodextrin makes me feel proud as it is the first paper of your bright young chemist Daniel Bisericaru, sprouting from the intense and fruitful collaboration between Francesco Trotta‘s team and Adrián Matencio Durán at Università degli Studi di Torino and CarboHyde.

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.

cyclodextrin, progesteron

Cyclodextrin encapsulation enabling the anticancer repositioning of disulfiram: Preparation, analytical and in vitro biological characterization of the inclusion 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.

This collaboration of Semmelweis University and Egis Pharmaceuticals PLC describes for the first time the complexation of disulfiram with randomly methylated-β-cyclodextrin.

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.

Cyclodextrin encapsulation enabling the anticancer repositioning of disulfiram: Preparation, analytical and in vitro biological characterization of the inclusion complexes – ScienceDirect

Wacker production site celebrates 25th Anniversary of manufacturing cyclodextrins

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®.

WACKER’s Eddyville Production Site Celebrates 25th Anniversary of Manufacturing Cyclodextrins for Global Customers (prnewswire.com)

Wacker

A novel process for the preparation of amorphous solid dispersion of 1-{3-[3-(4-chlorophenyl) propoxy] propyl} piperidine, hydrochloride with hydroxypropyl beta-cyclodextrin (HPBCD)

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.

In this patent by Biophore India Pharmaceuticals Pvt. Ltd. the combination of cyclodextrin and amorphous solid dispersion is discussed.

To learn more about such formulation strategies, check out our website: www.carbohydesolutions.com – Carbohyde

Espacenet – A NOVEL PROCESS FOR THE PREPARATION OF AMORPHOUS SOLID DISPERSION OF 1-{3-[3-(4-CHLOROPHENYL) PROPOXY] PROPYL} PIPERIDINE, HYDROCHLORIDE WITH HYDROXYPROPYL BETA-CYCLODEXTRIN (HPβCD)

Inclusion Complexes between β-Cyclodextrin and Gaseous Substances—N2O, CO2, HCN, NO2, SO2, CH4 and CH3CH2CH3: Role of the Host’s Cavity Hydration

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.

Inorganics | Free Full-Text | Inclusion Complexes between β-Cyclodextrin and Gaseous Substances—N2O, CO2, HCN, NO2, SO2, CH4 and CH3CH2CH3: Role of the Host’s Cavity Hydration (mdpi.com)

If you would like to learn more about such solutions, please visit: www.carbohydesolutions.com – Carbohyde

Development of Broad-spectrum β-cyclodextrins-Based Nanomaterials Against Influenza Viruses

Cyclodextrins as antivirals? Why not?

Caroline Tapparel VuFrancesco Stellacci and colleagues from EPFL and University of Geneva created a groundbreaking molecule, CD-SA, that mimics flu virus receptors to fight off multiple influenza strains effectively! 🦠💥 Our studies show CD-SA outperforms existing treatments like Oseltamivir, offering a new hope against flu with fewer chances of resistance when coupled with IFN λ1. Exciting results from lab to mice models prove its potent antiviral powers! 🚀🔬


Development of Broad-spectrum β-cyclodextrins-Based Nanomaterials Against Influenza Viruses | bioRxiv

Multifunctionality of cyclodextrin-based polymeric nanoparticulate delivery systems for chemotherapeutics, combination therapy, and theranostics

As cancer remains one of the most challenging diseases to treat, scientists have developed various medications and therapeutic approaches to combat it. To protect drugs from degradation or inactivation, efficient delivery systems are required during administration. In this context, cyclodextrin-based polymeric nanosystems have emerged as an effective treatment approach against cancer.

Cyclodextrins are natural oligosaccharides that can trap water-insoluble molecules inside their hydrophobic core, making them valuable in pharmaceutical research. When combined with polymeric nanoparticles, CD-based delivery systems provide versatile and tunable profiles, thanks to the submicron-sized PNPs. Recent studies have shown that CD-based delivery systems can successfully be applied in combination therapy and theranostics, providing multifunctional advantages against cancer.

The article by Lakshmi Sathi DeviCristina CasadidioMaria Rosa GigliobiancoPiera Di Martino and Roberta Censi from University of Camerino further discusses different binding approaches, release mechanisms of CD-drug complexation, and characterization studies. Promoting CD to a polymeric and nanoscale has demonstrated improved tumor targeting, reduced side effects, and prolonged drug release in preclinical studies and clinical trials. Notably, CD-based delivery systems, including CALAA-01, CRLX101, and CRLX301, have shown promising results in treating cancer.

Overall, cyclodextrin-based polymeric nanosystems hold great potential in tackling the abnormalities behind cancer by providing an efficient drug delivery system.

Multifunctionality of cyclodextrin-based polymeric nanoparticulate delivery systems for chemotherapeutics, combination therapy, and theranostics – ScienceDirect


METHOD FOR THE PRODUCTION OF LARGE-RING CYCLODEXTRINS

Today’s cyclodextrin is a great patent on unusual CDs: large-ringed ones. The systematic experimental study of the properties of the large-ring cyclodextrins (LR-CDs) as host systems was hampered for a long time by the inability to obtain individual LR-CDs in quantities necessary for experimental examinations. Breakthrough in the situation was a recent patent and reports of Sophie Beeren and coworkers from DTU – Technical University of Denmark

Now we have a scalable method, and the isolation of the product does not require chromatography. And what should we do with these CDs? Let’s start by looking into analytical, biotech, and pharma applications. Then we shall see…

WO2024042228 METHOD FOR THE PRODUCTION OF LARGE-RING CYCLODEXTRINS (wipo.int)

Combined use of nanobody, cyclodextrin and quercetin for protection from enveloped viruses

Fascinating antiviral application of cyclodextrins against SARS-COV2. You can find specific nanobodies against different target antigens such as the spike protein of the SARS-CoV-2 virus and or to the ACE2 receptor at the host cell surface, binds to the virus or the ACE2 receptor at the host cell plasma membrane, preventing entry of the SARS-CoV-2 virus. The nanobodies comprise a cyclodextrin; a zinc ionophore; a zinc-containing compound; and, benzalkonium.

WO2024035526 COMBINED USE OF NANOBODY, CYCLODEXTRIN AND QUERCETIN FOR PROTECTION FROM ENVELOPED VIRUSES (wipo.int)