Cluster Dextrin™

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.

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

The Story Behind Sugammadex’s Success

Few medical breakthroughs have been as transformative as Sugammadex. This remarkable drug, developed by the Dutch pharmaceutical company Organon, represents a significant milestone in anesthesia management, particularly in reversing the effects of neuromuscular blockade.

The journey of Sugammadex began with the quest to address the limitations of traditional methods for reversing muscle relaxation induced by anesthesia. These methods often involve lengthy processes with unpredictable outcomes and potential side effects. Recognizing the need for a safer, more efficient solution, researchers turned their attention to cyclodextrins.

Cyclodextrins are a family of cyclic oligosaccharides characterized by a hydrophobic interior and a hydrophilic exterior. Their unique structure enables them to encapsulate guest molecules, forming inclusion complexes. This property intrigued scientists, leading to the exploration of cyclodextrins as potential candidates for reversing neuromuscular blockade.

Among cyclodextrins, gamma-cyclodextrin emerged as a promising candidate due to its ability to encapsulate the neuromuscular blocking agents rocuronium and vecuronium. Building upon this discovery, Organon researchers synthesized Sugammadex, a modified gamma-cyclodextrin specifically designed to encapsulate rocuronium and vecuronium with high affinity.

The first occurrence of Sugammadex in the scientific literature can be traced back to a pivotal study published in 2001. This groundbreaking research, titled “Org 25969, a Novel, Specific Reversal Agent for Rocuronium-Induced Neuromuscular Blockade,” was conducted by researchers from Organon, the pharmaceutical company that developed Sugammadex.

In this study, the authors introduced Sugammadex, then known as Org 25969, as a novel reversal agent for rocuronium-induced neuromuscular blockade. They demonstrated its efficacy in rapidly and effectively reversing the effects of rocuronium, a commonly used neuromuscular blocking agent during anesthesia. This publication laid the foundation for subsequent research and clinical trials that ultimately led to the approval and widespread adoption of Sugammadex as a critical tool in anesthesia management.

Since its initial introduction in scientific literature, Sugammadex has been the subject of numerous studies, reviews, and clinical trials, further validating its efficacy and safety in clinical practice. Its discovery marked a significant advancement in anesthesia pharmacology and continues to benefit patients undergoing surgical procedures worldwide.

The development of Sugammadex was not without challenges. Regulatory hurdles and safety concerns necessitated extensive testing and refinement. However, the perseverance of the research team eventually paid off, culminating in the approval of Sugammadex for clinical use in various countries.

The impact of Sugammadex on anesthesia practice cannot be overstated. Its rapid and reliable reversal of neuromuscular blockade offers numerous advantages, including shorter recovery times, improved patient safety, and enhanced control for medical professionals. By streamlining procedures and minimizing risks, Sugammadex has revolutionized anesthesia management, setting a new standard of care in the field. Currently, it is a blockbuster drug marketed by MSD and developed by dozens of generic companies.

In summary, Sugammadex represents the convergence of scientific ingenuity, perseverance, and innovation. Its development underscores the pivotal role of cyclodextrins in drug discovery and highlights the transformative potential of research-driven solutions in improving patient outcomes.

Would you like to learn more? Here are some great sources to start with!

Org 25969 (sugammadex), a selective relaxant binding agent for antagonism of prolonged rocuronium-induced neuromuscular block

Preclinical pharmacology of sugammadex

EMA submission document

Sugammadex – A revolutionary drug in neuromuscular pharmacology

Isosorbide mononitrate spray and preparation method

Today’s cyclodextrin is an innovative formulation of isosorbide mononitrate. In this patent, a cyclodextrin complex is prepared, suitable to develop sprays, having the advantages of quick response, small irritation, and convenience in use.

Isosorbide mononitrate is a medication primarily used for the prevention of angina pectoris, which is chest pain caused by reduced blood flow to the heart. It works by relaxing and widening blood vessels, which allows more blood and oxygen to reach the heart, thereby reducing the heart’s workload and helping to prevent episodes of chest pain. It belongs to a class of drugs known as nitrates.

Isosorbide mononitrate is used in a long-acting form, which is not suitable for relieving an acute angina attack but is used regularly to decrease the frequency and severity of angina episodes. It may also be used in other conditions as determined by a doctor, based on its vascular effects.

It is typically available in tablet form for oral administration. This medication is taken by mouth and is formulated as either immediate-release or extended-release tablets, depending on the intended dosing schedule and therapeutic need. The drug acts by releasing nitric oxide, which helps to relax and widen blood vessels, but the drug itself is solid in its delivery form.

Espacenet – Isosorbide mononitrate spray and preparation method thereof

Monitoring the conformational ensemble and lipid environment of a mechanosensitive channel under cyclodextrin-induced membrane tension

Today’s cyclodextrin from Christos Pliotas form The University of Manchester research reveals new insights into the activation kinetics of mechanosensitive channels. By mimicking tension through the sequestering of lipids from membranes, cyclodextrins enable the conversion of mechanical cues into electrical signals. The extent of MscS activation depends on the cyclodextrin-to-lipid ratio, with lipids being depleted slower when MscS is present.

This has implications for the activation kinetics of MscS in different membrane scaffolds. Additionally, MscS transits from closed to sub-conducting state(s) before it desensitizes due to the lack of lipid availability in its vicinity required for closure.

This approach allows for monitoring tension-sensitive states in membrane proteins and screening molecules capable of inducing molecular tension in bilayers.

Monitoring the conformational ensemble and lipid environment of a mechanosensitive channel under cyclodextrin-induced membrane tension: Structure (cell.com)

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

Mirror-image cyclodextrins

today’s cyclodextrin:
Do you often take a good look in the mirror?

Nobel laureate Sir Fraser Stoddard, Daniel W. Armstrong, and their team report the syntheses of three mirror-image CDs—namely, α-, β- and γ-L-CDs, which are composed of six, seven and eight α-1,4-linked L-glucopyranosyl residues, respectively.

The availability of L-CDs has enabled the elucidation of an unprecedented chiral self-sorting of a racemic modification of β-CDs in the solid state and an investigation of the chiral recognition of enantiomeric fenchone by α-L-CD. This research identifies a missing piece of the cyclodextrin jigsaw and sets the stage for scientists to explore the mirror-image world of naturally occurring CDs.

Mirror-image cyclodextrins | Nature Synthesis

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)

Drugs in Cyclodextrin in Liposomes: How a Suitable Formulation of an Active Substance Can Improve Its Efficiency?

today’s cyclodextrin:
Drugs in Cyclodextrin in Liposomes: How a Suitable Formulation of an Active Substance Can Improve Its Efficiency?

Great paper from Prof Geraldine Gouhier, François Estour and colleagues from Université de Rouen on the design of new drug delivery systems.

Liposome formulations are pivotal in medicine for their ability to improve drug solubility, allowing for targeted delivery directly to disease sites, which minimizes side effects. They enable controlled and sustained release of medications, reducing dosage frequency. Their ability to encapsulate a variety of substances makes them versatile for different treatments, significantly reducing toxicity and enhancing the stability of drugs, especially sensitive biological compounds. This ensures a more effective and safer therapeutic approach.

Discover how the innovative “drug-in-cyclodextrin-in-liposomes” method is revolutionizing drug delivery! Enhancing drug stability & release, this latest review dives into how these nano-carriers improve the efficacy of various drugs. 🧬💊

Processes | Free Full-Text | Drugs in Cyclodextrin in Liposomes: How a Suitable Formulation of an Active Substance Can Improve Its Efficiency? (mdpi.com)