Uses of cyclodextrin polymers.

Today's cyclodextrin, drug development

How about a case study now?From bacterial toxin to long-acting pain relief

Challenge: Chronic & neuropathic pain still largely rely on short-acting, addictive opioids.

Innovation: A β-cyclodextrin polymer that encapsulates mycolactone, turning an insoluble, UV-sensitive molecule into a stable, aqueous formulation.

Chemistry: Crosslinked β-CD forms multiple host–guest cavities, solubilising and protecting mycolactone without organic solvents.

Impact: In vivo, the pCD–mycolactone combo delivers strong, long-lasting analgesia from a single injection — a promising non-opioid alternative for difficult-to-treat pain.

Check out the patent in comments if you like the idea of Ruxandra Gref; Isabelle Marsollier and Estelle Marion. We do so!

Espacenet – LONG-ACTING PAIN-RELIEF FORMULATION

Would you like to design a similar polymer for you application? Let us know, we can help.

Sugammadex – Alfaxalone?

drug development,

Present: Sugammadex can be used to reverse rocuronium and similar NMBA.
The future: Alfaxalone?

This rat study shows that Sugammadex can reverse the anesthetic effects of alfaxalone.

Recovery speed from alfaxalone anesthesia is dependent upon sugammadex dose and sex.

Obviously, its not working as well as for the original target (Compared to saline controls, sugammadex shortened recovery times by 40%–60% following anesthesia induction) but the repurposing idea is nice.

What do you think? Can a scavenger like this be repurposed for other applications?

Use of Sugammadex to Reverse Alfaxalone Anesthesia in Rats – ScienceDirect

Enantioselective Complexation of Xylopinine: A Cyclodextrin-Assisted CE and NMR Study

Today's cyclodextrin, drug development, ,

Xylopinine (XPN) a natural cytotoxic, antimicrobial, and antimalarial compound
fits cyclodextrins well!

Milo Malanga PhD‘s latest collaboration with Semmelweis University (Erzsébet Várnagy, Fejős Ida, Tóth Gergő) and Eötvös Loránd University (Szabolcs Béni) shares insights into the encapsulation behavior:

Some cyclodextrins like subetadex provide excellent enantiomer resolution and could be key agents for quality control.

Enantioselective Complexation of Xylopinine: A Cyclodextrin-Assisted CE and NMR Study

Hydroxypropyl-Beta-Cyclodextrin (HP-BCD) inhibits SARS-CoV-2 replication

Today's cyclodextrin, drug development,


This study brings some fascinating highlights:

1. HP-BCD impacts cellular ACE2 distribution and early SARS-CoV-2 replication.

2. HP-BCD alters cholesterol and lipid droplets content and organization.

3. HP-BCD impairs viral compartments formation in SARS-CoV-2-infected cells.

4. HP-BCD affects both early and late stages of SARS-CoV-2 replication.

5. HP-BCD inhibition of SARS-CoV-2 is partially reversed by cholesterol replenishment.

Which do you think is the most impactful?

Hydroxypropyl-Beta-Cyclodextrin (HP-BCD) inhibits SARS-CoV-2 replication by modulating intracellular lipid dynamics and preventing viral replication complex formation – ScienceDirect

No cholesterol – no pain?

Today's cyclodextrin, drug development,

Let’s start the week with an amazing Hungarian paper from University of Pécs.

Cyclodextrin (CD) derivatives deplete cholesterol from membrane rafts in TRPV1 and TRPA1 channels, reducing receptor activation in vitro, anticipating in vivo analgesic effects.

The tested CD derivatives are promising agents for exerting peripheral analgesia and anti-inflammation via cholesterol depletion, also supported by in vitro and in silico findings.

Andrea Nehr-Majoros, Maja Payrits, Noémi Bencze, GYORGY SETALO JR, Rita Börzsei, Csaba Hetényi, Zsuzsanna Helyes, Éva Szőke

Cyclodextrins inhibit TRPV1 and TRPA1 activation-induced nociception via cholesterol depletion – Journal of Lipid Research

Selective removal of 7-ketocholesterol by a novel atherosclerosis therapeutic candidate reverts foam cells to a macrophage-like phenotype

Today's cyclodextrin, drug development,

Today’s cyclodextrin:

Say hello to Cyclarity Therapeutics‘s UDP-003, a promising new therapeutic that goes beyond managing atherosclerosis — it aims to reverse it by targeting one of its nastiest culprits: 7-ketocholesterol (7KC), a toxic oxidized form of cholesterol. 🧨🧬

Here’s what the science says:
🧼 UDP-003 selectively removes 7KC, a molecule notorious for turning immune cells into dysfunctional foam cells — the building blocks of atherosclerotic plaque
🔄 By clearing out 7KC, foam cells regain their phagocytic power and reduce harmful features like oxidative stress and lipid accumulation
🧲 The treatment downregulates CD47, a “don’t eat me” signal, and restores efferocytosis, helping clean up dead cells in plaques
🚽 7KC is not just neutralized — it’s flushed out via urine, suggesting effective systemic detox
✅ Preclinical safety looks good, and a Phase 1 clinical trial is already underway!

💡 Bottom line: By targeting the molecular root — not just the symptoms — of atherosclerosis, UDP-003 could become the first truly disease-modifying therapy for this global cardiovascular killer 🛡️❤️

Selective removal of 7-ketocholesterol by a novel atherosclerosis therapeutic candidate reverts foam cells to a macrophage-like phenotype – Atherosclerosis

HPBCD will be dosed in patients with diabetic kidney disease in Q2 2025

Today's cyclodextrin, drug development, ,

Today’s cyclodextrin:
ZyVersa Therapeutics Inc.‘ Cholesterol Efflux Mediator VAR 200 (HPBCD) will be dosed in patients with diabetic kidney disease in Q2 2025.

The first patient is expected to be treated in a phase 2a clinical trial in patients with DKD by the end of June of 2025. The intent of the study is to obtain renal patient proof-of-concept for VAR 200 prior to initiating a larger phase 2a/b for VAR 200’s lead indication, FSGS. The DKD study will evaluate VAR 200’s safety and efficacy (% change in proteinuria from baseline to week 12) in eight patients with type 2 diabetes who have diabetic kidney disease. This data will provide insights for designing the subsequent phase 2a/b FSGS study. The DKD study will be conducted at two clinical research sites.

I cannot wait to see how this goes!
ZyVersa Therapeutics Reports First Quarter 2025 Financial Results and Highlights Pipeline Progress :: ZyVersa Therapeutics, Inc.

Fascinating Hungarian invention in ophthalmic application

drug development,

After oral and parenteral formulation, ophthalmics are the 3rd most popular for cyclodextrin use.

Here is a fascinating Hungarian invention in the field of ophthalmology from Semmelweis University and University of Szeged.

US20250108034 EYE DROP FORMULATION

An ocular formulation comprising a cyclodextrin-formulated L-Ascorbic acid 6-palmitate (ASP), preferably for the treatment of fibrosis in the cornea, corneal haze, and wound.

Heartiest congratulations to György Tibor Balogh, PhD, DSc, dr. habil and his team and Gábor Katona, Ildiko Csoka and their team.

We hope to see many more of similar great solutions to come!

Optimizing 6-benzylaminopurine for micropropagation: A cyclodextrin monomers and polymers approach

education, drug development, Non-pharma applications, ,

What a personal milestone!

Our youngest one, Dani Bisericaru was still at Università degli Studi di Torino when he did this work that now led to his first first-author paper.

Special gratitude goes to Francesco Trotta and Adrián Matencio Durán for their excellent mentorship of Dani that we enjoy to this very day at CarboHyde.

So check out and learn how this research lays the foundation of the eco-friendly use of cyclodextrin-based polymers for micropropagation improvement.

Optimizing 6-benzylaminopurine for micropropagation: A cyclodextrin monomers and polymers approach – ScienceDirect

Exceptional stability of the sugammadex-solasodine complex: Insights from experimental and theoretical studies

drug development

A new paper out!

Sugammadex (SGM) is the first cyclodextrin (CD)-based selective relaxant binding agent. We investigated its ability to capture natural aminosteroid phytotoxins, and assessed its potential as an antidote for intoxication.

SGM significantly increased cell survival and reduced Solasodine (the toxic alkaloid chosen as model compound) toxicity in mHippoE-14 mouse hippocampal embryonic cells, supporting the hypothesis that SGM could act as an antidote to SS’s toxic effects.

Special thanks for the fantastic teamwork:
Eszter Kalydi – Semmelweis University
Fanni Sebák, Éva Moussong József Kardos, Andrea Bodor Szabolcs Béni – Eötvös Loránd University
Béla Fiser – University of Miskolc
Babak Minofar – University of Lodz
Milo Malanga PhD – CarboHyde

Exceptional stability of the sugammadex-solasodine complex: Insights from experimental and theoretical studies – ScienceDirect