α-Cyclodextrin supplementation improves endurance exercise performance and reduces post-exercise fatigue in human males

Today's cyclodextrin

ONE way to boost your performance!

Today’s cyclodextrin is another clinical study showing the benefits of using alpha-cyclodextrin to improve exercise performance and reduces post-exercise fatigue.

α-Cyclodextrin (αCD), a cyclic hexasaccharide composed of six glucose units, is not digested in the small intestine but is completely fermented by gut microbes.

αCD supplementation significantly improved endurance exercise performance (10 km biking time trial) compared with the placebo.

The heart rate increase was lower in the αCD group than in the placebo group during exercise.

α-Cyclodextrin supplementation improves endurance exercise performance and reduces post-exercise fatigue in human males: a randomized, double-blind, placebo-controlled, parallel-group study (jst.go.jp)

Advances in Cyclodextrins and Their Derivatives in Nano-Delivery Systems

Today's cyclodextrin,

Today’s cyclodextrin is an easy review on Advances in Cyclodextrins and Their Derivatives in Nano-Delivery Systems

The areas covered include nanospheres, nano-sponges, nanogels, cyclodextrin metal–organic frameworks, liposomes, and emulsions, providing a comprehensive and in-depth understanding of the design and development of nano-delivery systems.

Advances in Cyclodextrins and Their Derivatives in Nano-Delivery Systems (mdpi.com)

Encapsulation of 5-fluorouracil in cholesteryl-modified cyclodextrin: thermal, spectral, and computational assessment of drug inclusion efficiency

drug development, Today's cyclodextrin

Today’s cyclodextrin:
I have seen many visualizations and artwork of cyclodextrins so far, yet this “jellyfish” cover caught my eye.

Cholesteryl-modified cyclodextrin (also a great idea) to capture and deliver 5-fluorouracil.

Encapsulation of 5-fluorouracil in cholesteryl-modified cyclodextrin: thermal, spectral, and computational assessment of drug inclusion efficiency – Journal of Materials Chemistry B (RSC Publishing)

COMPOSITIONS OF HYDROXYPROPYL-BETA-CYCLODEXTRIN AND METHODS OF PURIFYING THE SAME

Today's cyclodextrin

Today’s cyclodextrin is yet another fascinating patent from Beren Therapeutics, and my old colleague, Gábor Benkovics PhD on HPBCD.

This time they show methods of isomerically purifying a mixture of hydroxypropyl-β-cyclodextrins, with the goal of creating safer and better active ingredients from “common” cyclodextrins.

Way to go guys!

Beren’s former patents detailed the use of HPBCD in various hashtag#cardiovascular conditions involving hashtag#cholesterol homeostasis such as hashtag#atherosclerosis or familiar hypercholesterolemia.

US20240270877 COMPOSITIONS OF HYDROXYPROPYL-BETA-CYCLODEXTRIN AND METHODS OF PURIFYING THE SAME (wipo.int)

Axsome Therapeutics Announces FDA Acceptance of NDA Resubmission for AXS-07 for the Acute Treatment of Migraine

drug development, Today's cyclodextrin

Today’s cyclodextrin update brings news of the 2nd oral drug to be marketed using sulfobutylether-beta-CD.

Axsome Therapeutics, Inc. has announced that the U.S. FDA has acknowledged the resubmission of the NDA for AXS-07, an oral, rapidly absorbed, multi-mechanistic investigational medicine for the acute treatment of migraine. AXS-07 combines MoSEIC™ meloxicam and rizatriptan, offering a new molecular entity for migraine treatment enabled by Axsome’s innovative technology.

About Migraine
Migraine is a serious neurological condition characterized by recurrent attacks of pulsating, often severe and disabling head pain associated with nausea, sensitivity to light, and sensitivity to sound. An estimated 39 million Americans suffer from migraine, and it is the leading cause of disability among neurological disorders in the United States according to the American Migraine Foundation. Published surveys of migraine sufferers found that more than 70% are not fully satisfied with their current treatment and desire therapies that work faster, more consistently, and result in less symptom recurrence.

About AXS-07
AXS-07 is a novel, oral, rapidly absorbed, multi-mechanistic investigational medicine for the acute treatment of migraine, consisting of MoSEIC™ meloxicam and rizatriptan. Meloxicam is a new molecular entity for migraine enabled by Axsome’s MoSEIC (Molecular Solubility Enhanced Inclusion Complex) technology, which results in rapid absorption of meloxicam while maintaining a long plasma half-life. Meloxicam is a COX-2 preferential non-steroidal anti-inflammatory drug and rizatriptan is a 5-HT1B/1D agonist. AXS-07 is designed to provide rapid, enhanced and consistent relief of migraine, with reduced symptom recurrence. AXS-07 is covered by more than 200 issued U.S. and international patents which provide protection until at least 2038. AXS-07 is not approved by the FDA.

Axsome Therapeutics Announces FDA Acceptance of NDA Resubmission for AXS-07 for the Acute Treatment of Migraine | Axsome Therapeutics, Inc. (gcs-web.com)

Role of Cyclodextrin Cross-Linker Type on Steroid Hormone Micropollutant Removal from Water Using Composite Nanofiber Membrane

Today's cyclodextrin

Today’s cyclodextrin is about water purification.

What if we could make our water cleaner using a safer, composite nanofiber membrane?

This study investigates how different cross-linkers affect the stability and micropollutant removal efficiency of β-cyclodextrin polymers in composite nanofiber membranes. It finds that triphenylolmethane triglycidyl ether (TPTE) and trimethylolpropane triglycidyl ether (TMTE) are effective alternatives to the more toxic epichlorohydrin (EP) for removing steroid hormones from water.

Check out the paper by Han-Ya Lin (with Akhil Gopalakrishnan, PhD in the photo) et al., “Role of Cyclodextrin Cross-Linker Type on Steroid Hormone Micropollutant Removal from Water Using Composite Nanofiber Membrane,” here: https://lnkd.in/diXpHPWK

Role of Cyclodextrin Cross-Linker Type on Steroid Hormone Micropollutant Removal from Water Using Composite Nanofiber Membrane | ACS Applied Polymer Materials

Cyclodextrins: Establishing building blocks for AI-driven drug design by determining affinity constants in silico

Today's cyclodextrin,

Today’s cyclodextrin:
Check out this fascinating paper guiding us to the future of CDs:

AI-driven cyclodextrin drug design

Fascinating research by Amelia Anderson & Matthew “Oki” O’Connor from Cyclarity Therapeutics and Angel Piñeiro & Rebeca Garcia-Fandino from Universidad de Santiago de Compostela

Computational methods represent an exceptional complement to in vitro assays because they can be employed for existing and hypothetical molecules, providing high resolution structures in addition to a mechanistic, dynamic, kinetic, and thermodynamic characterization.

Bridging computational methods with complex molecular interactions, this research enables predictive CD designs for diverse applications. Moreover, the high reproducibility, sensitivity, and cost-effectiveness of the studied methods pave the way for extensive studies of massive CD-ligand combinations, enabling AI algorithm training and automated molecular design.

Cyclodextrins: Establishing building blocks for AI-driven drug design by determining affinity constants in silico – Computational and Structural Biotechnology Journal (csbj.org)

Preparation of Carvacrol β-Cyclodextrin Inclusions and 1-Methylcyclopropene-α-CD Coated Paper by Water-Free Method for Postharvest Preservation of Peach

Today's cyclodextrin

Today’s cyclodextrin: is a packaging/food preservation application

Where Carvacrol β-Cyclodextrin Inclusions and 1-Methylcyclopropene-α-CD Coated Paper are for post-harvest preservation of peach.

Carvacrol essential oil has broad-spectrum antibacterial properties, but it is volatile and unstable for long-term storage and use. In the present study, carvacrol was encapsulated with β-cyclodextrin to improve its relevant properties.

PEG was used to form the film in the anhydrous condition, and the compound and ethylene inhibitor 1-methylcyclopropene (1-MCP) were included to obtain the film-coated paper.

This study provides a solution for preparing controlled-release coated paper with essential oils and 1-MCP bioactives to extend the shelf life of fruits and vegetables.

Preparation of Carvacrol β-Cyclodextrin Inclusions and 1-Methylcyclopropene-α-CD Coated Paper by Water-Free Method for Postharvest Preservation of Peach | Food and Bioprocess Technology (springer.com)

β-Cyclodextrin nano-encapsulated carvacrol inclusion complexes improve postharvest quality of limes (Citrus latifolia Tanaka) (usda.gov)

Reusable Cyclodextrin-Mediated Electrochemical Sensor in Automated Flow Cell for Cortisol Detection

Today's cyclodextrin,

Today’s cyclodextrin is detecting cortisol.

It comes from the oven of Ferdows Sajedi and Jeffrey Halpern at University of New Hampshire. The focus is on using beta-cyclodextrin (βCD) to electrochemically detect cortisol employing an automated flow cell system.

The ultimate goal is to optimize sensor stability, sensitivity, and reproducibility, contributing to the advancement of cortisol detection with the automated cyclodextrin-mediated biosensors.

Reusable Cyclodextrin-Mediated Electrochemical Sensor in Automated Flow Cell for Cortisol Detection – IOPscience

Oculis closes Phase 3 eye drop trial due to ‘administrative error’ from third party

Today's cyclodextrin,

Today’s cyclodextrin is some news fresh from Oculis‘s oven about the lead drug OCS-01, which is delivered with a unique and proprietary cyclodextrin technology.

The company reported in its second-quarter financial filing that a Phase 3 trial for Oculis’ lead eye drop candidate will be shut down due to an administrative error.

The company added, however, that it had a pre-NDA meeting with the FDA this month, where it got the go-ahead to still file for approval in the first quarter of next year. According to Oculis, the agency confirmed the data it already has from its first Phase 3 trial and a Phase 2 trial, alongside safety data from other studies in ocular surgery and diabetic macular edema, are enough to support an NDA submission.

I’m so happy that this unfortunate event does not seem to hold back the progress of this amazing drug and technology.

If OCS-01 is approved, it would be the first daily and preservative-free steroid for treating inflammation and pain following ocular surgery.