Pharmaceutical composition and application patent

Today’s cyclodextrin is an interesting application proposed by RemeGen Biosciences, which uses methyl-BCD to remarkably improve the pharmaceutical effect of antibody-drug conjugates. By using CDs, the ACD load can be lower, thus greatly reducing the production cost and the treatment cost of a patient.
If you are interested in similar solutions, check out Formulation development – www.carbohydesolutions.com

Espacenet – Pharmaceutical composition and application thereof

Synthesis and Preliminary Evaluation of an ASGPr-Targeted Polycationic β-Cyclodextrin Carrier for Nucleosides and Nucleotides

As our interest to use cyclodextrin in genetherapy as superior drugdelivery tools continue, we welcome papers like this, where cationic CD polymers are used for nucleotide formulation.
Leonard Wiebe and coworkers from University of Alberta development a carrier designed to effect selective transmembrane internalization of nucleotides via the asialoglycoprotein receptor.

Pharmaceutics | Free Full-Text | Synthesis and Preliminary Evaluation of an ASGPr-Targeted Polycationic β-Cyclodextrin Carrier for Nucleosides and Nucleotides (mdpi.com)


Hydroxypropyl-Beta Cyclodextrin Barrier Prevents Respiratory Viral Infections: A Preclinical Study

Hydroxypropyl-Beta Cyclodextrin Barrier Prevents Respiratory Viral Infections: A Preclinical Study

In this work form University of Southern California blocking viral attachment and entry at the nasal airway using a cyclodextrin-based formulation is presented, so that a preventative therapy can be developed to reduce viral infection at the site of entry. After screening several CDs, hydroxypropyl beta-cyclodextrin (HPBCD) and hydroxypropyl gamma-cyclodextrin (HPGCD) were then further evaluated for antiviral effects using SARS-CoV-2 pseudotypes. Intranasal pre-treatment with HPBCD-based formulations reduced viral load and inflammatory signaling in the lung.

In vitro efficacy studies were further conducted using lentiviruses, murine hepatitis virus (MHV), and influenza A virus subtype H1N1. These findings suggest HPBCD may be used as an agnostic barrier against transmissible pathogens, including but not limited to SARS-CoV-2.

IJMS | Free Full-Text | Hydroxypropyl-Beta Cyclodextrin Barrier Prevents Respiratory Viral Infections: A Preclinical Study (mdpi.com)

New cyclodextrin dimer patent!

today’s cyclodextrin:
I am proud to share this new patent from Cyclarity Therapeutics not only because of the fantastic chemistry and excellent drug development but also as CarboHyde CSO Milo Malanga is among the inventors!

Cyclodextrin dimers are used to target 7-ketocholesterol, eventually to reverse atherosclerotic plaques.
Check out for more info: Espacenet – US2024043661A1

Congratulation to Milo and the geat team at Cyclarity!

Oral alpha-cyclodextrin reverses cholesterol-crystal-induced retinal pathology in a rodent model of type 2 diabetes

Today’s cyclodextrin a study showing how alpha-CD treatment could be used in type-2 diabetes patients.
Cholesterol crystals were eliminated from the retinas of diabetic mice after oral alpha-cyclodextrin treatment. These findings demonstrate that T2D is associated with cholesterol crystal-induced retinal pathology that is improved using oral alpha-cyclodextrin. Improvements were observed in inflammation, neural function and visual response.

Oral alpha-cyclodextrin reverses cholesterol-crystal-induced retinal pathology in a rodent model of type 2 diabetes (T2D). | IOVS | ARVO Journals

New Captisol (Ligand Pharmaceuticals) enabled API on the market!

Today’s cyclodextrin:

Eisai Co., Ltd. obtained marketing authorization approval in January 2024 from the Japanese Ministry of Health, Labour and Welfare for the injection formulation of its in-house discovered antiepileptic drug (AED) Fycompa® (perampanel) in Japan as an alternative therapy when oral administration is temporarily not possible. Fycompa is formulated with Captisol®, a Ligand technology.

About perampanel (Fycompa®)
Perampanel is a first-in-class anti-epileptic agent (AED) discovered and developed by Eisai. With epileptic seizures being mediated by the neurotransmitter glutamate, the agent is a highly selective, noncompetitive AMPA receptor antagonist that reduces neuronal hyperexcitation associated with seizures by targeting glutamate activity at AMPA receptors on postsynaptic membranes. Perampanel is currently approved in more than 75 countries and territories, including Japan, China, and other countries in Europe and Asia, as an adjunctive treatment for partial-onset seizures (with or without secondarily generalized seizures) in patients with epilepsy 12 years of age and older. In addition, perampanel has been approved in more than 70 countries, including Japan, Europe, and Asia, for treatment as an adjunctive therapy for primary generalized tonic-clonic seizures in patients with epilepsy 12 years of age and older. In Japan and China, perampanel is approved for monotherapy and adjunctive use in the treatment of partial-onset seizures (with or without secondarily generalized seizures) in patients with epilepsy 4 years of age and older. In Europe, the approved age range is 4 years of age and older for the adjunctive treatment of partial-onset seizures (with or without secondarily generalized seizures) and 7 years of age and older for the treatment as an adjunctive therapy for primary generalized tonic-clonic seizure. A tablet, fine granule formulation, and injection formulation have been approved in Japan. An oral suspension formulation and tablet have been approved in Europe and China. In January 2023, the commercial rights in the United States were transferred to Catalyst Pharmaceuticals, Inc.

Stable, liquid pharmaceutical compositions comprising Melphalan

The cyclodextrin-enabled formulation of melphalan is an excellent example of how outdated excipients could be replaced with safer and more effective cyclodextrins to create patient-friendly and superior drug products!
Espacenet – Stable, liquid pharmaceutical compositions comprising melphalan
here you can find similar examples: Formulation development – www.carbohydesolutions.com

Functionalization of cotton nonwoven with cyclodextrin/lawsone inclusion complex nanofibrous coating for antibacterial wound dressing

Today’s cyclodextrin is a new type of wound dressing developed at Cornell University by Tamer Uyar‘s team.

Bioactive compounds like lawsone offer dual benefits of wound healing and infection prevention, however, their limited solubility and viability hinder their applications. To address this, Hydroxypropyl-beta-cyclodextrin (HP-β-CD) and Hydroxypropyl-gamma-cyclodextrin (HP-γ-CD) were employed.

Electrospinning yielded smooth and uniform nanofibers with an average diameter of ∼300–700 nm. The nanofibers exhibited ∼100 % loading efficiency of lawsone and its rapid release upon dissolution.

Notably, antibacterial assays demonstrated the complete elimination of Escherichia coli and Staphylococcus aureus colonies. The CD/lawsone nanofibers also showed suitable antioxidant activity ranging from 50% to 70%.

Functionalization of cotton nonwoven with cyclodextrin/lawsone inclusion complex nanofibrous coating for antibacterial wound dressing – ScienceDirect

Comparative investigation of pulmonary vasodilating effects of inhaled Nitric Oxide (NO) gas therapy and inhalation of SIN-1, a new drug formulation containing an NO-donor metabolite

Today’s cyclodextrin is a nice collaborative formulation and in vivo (porcine) study between Semmelweis University and Cyclolab R&D Ltd.
In the project, the hemodynamic effect of inhalative SIN-1a (the unstable active metabolite of molsidomine, stabilized by cyclodextrine) was studied. The pulmonary vasodilator effect of SIN-1 was dose dependent, and in case of larger dose it was comparable to that of iNO. However, the vasodilatory effects of SIN-1 inhalation was not limited to the pulmonary circulation, a significant and dose-dependent systemic vasodilation could also be documented.
My only regret here is not all contributors met the authors’ list finally.

Comparative investigation of pulmonary vasodilating effects of inhaled Nitric Oxide (NO) gas therapy and inhalation of SIN-1, a new drug formulation containing an NO-donor metabolite | European Heart Journal | Oxford Academic (oup.com)

Cyclodextrin-Enabled Enantioselective Complexation Study of Cathinone Analogs

We have a nice read to propose for the week-started coffee, the most recent work of Szabolcs Béni from our advisory board and András DohárszkyFejős IdaEszter Kalydi and Gergely Völgyi.
A comprehensive investigation of the stability of cathinone derivatives and their cyclodextrin complexes.

Molecules | Free Full-Text | Cyclodextrin-Enabled Enantioselective Complexation Study of Cathinone Analogs (mdpi.com)