Cyclodextrin as a green anti-agglomerate agent in oil-water emulsion containing asphalt

Today's cyclodextrin, , ,

University of Science and Technology Beijing presents a very unique use of CDs:
Anti-agglomerate agents (AAs) are a cost-effective method to prevent hydrates from clogging submarine oil/gas pipelines. However, conventional AAs such as Span 80 is not applicable in oil/gas pipelines rich in asphalt because asphalt is easy to occupy the binding sites on the water droplet surface. On the other hand, CDs show excellent anti-agglomerate characteristics in oil–water systems containing asphalt by forming stable hydrogen bonds with water molecules. Compared with Span 80, the initial contact time between water droplets and hydrate is delayed by five times after adding CD molecules. CD-asphalt interaction prevents water droplets from spreading on the hydrate surface by maintaining the stability of the emulsion.
The unique properties of CD provide a molecular basis for developing more green and efficient AAs.

See the full article here.


Mannose-methyl-β-cyclodextrin suppresses tumor growth by targeting both colon cancer cells and tumor-associated macrophages

drug discovery, ,

Last week we shared applications of cyclodextrin in various types of cancer, and a discussion was triggered byTamas Sohajda about “why is it always HPBCD that is studied.” In this paper from Kumamoto University, JAPAN, by Keiichi Motoyama, Mannose-methyl-β-cyclodextrin is applied to suppress tumor growth by targeting colon cancer cells and tumor-associated macrophages.

See the full article here.

Hydroxypropyl-β-cyclodextrin inhibits the development of triple-negative breast cancer by enhancing antitumor immunity

drug development, ,

After sharing news on treating lymphedema, we came across another potential therapeutic use of cyclodextrin. In this preprint from Hefei University of Technology and Emory University authors demonstrate that 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) inhibited the growth and metastasis of triple-negative breast cancer (TNBC) both in vitro and in vivo, although the underlying mechanisms are unclear.
Cholesterol supplementation can attenuate HP-b-CD-inhibited TNBC growth and metastasis both in vitro and in vivo. In vivo, HP-β-CD promoted the infiltration of T cells into the tumor microenvironment (TME) and improved the exhaustion of CD8+ T cells via reducing endoplasmic reticulum (ER) stress and immune checkpoint molecules. Additionally, HP-β-CD inhibited the recruitment of tumor-associated macrophages to the TME by reducing the CCL2-p38MAPK-NF-kB axis. HP-β-CD also inhibited the epithelial-mesenchymal transition (EMT) of TNBC cells mediated by transforming the growth factor-b (TGF-b) signaling pathway.
In summary, the data in the current study suggest that HP-β-CD effectively inhibited the proliferation and metastasis of TNBC and melanoma, highlighting HP-β-CD may be a potential general antitumor clinical drug.

See the full article here

The authors found that HP-b-CD inhibits the proliferation and metastasis of TNBC by reducing cholesterol levels. HP-b-CD promotes T cell recruitment to the TME and improves CD8+ T cell exhaustion. Additionally, HP-b-CD inhibits TAMs accumulation.

Methyl-BCD is used in antibody-drug conjugate

Today's cyclodextrin, ,

An interesting application is highlighted in the patent of RemeGen荣昌生物: methyl-BCD is used in antibody-drug conjugate formulations where the primary benefit is that ADC dose can be lowered (due to higher efficacy), which leads to mitigating safety concerns lowering costs, and patient treatment costs. Fascinating, huh? (Figure: Araris Biotech AG)

See the full patent on Espacenet.


β and γ-Cyclodextrin dimers: design, characterization and in silico studies to explore the cooperative effect of the cavities

carbohydrates, drug delivery

This is a real delicacy for #carbohydrates and #cyclodextrin lovers from the group of Graziella Vecchio – Università di Catania (Luana La Piana, Livia Basile, Chiara Ragusa et al.). They synthesize and characterize two new β and γ-cyclodextrin dimers and compare their complexation behavior. The two cavities in the same molecule significantly improve the stability of inclusion complexes – particularly investigated cholic acid, cholesterol, and doxorubicin as guests.

See the full article here.

Method for stabilizing the pH of an aqueous composition comprising a drug

Today's cyclodextrin,

While the mainstream use of CDs in pharma is solubilization, improving chemical stability is close to 2nd most popular, even though it is more complicated to achieve. This patent by Thorsteinn Loftsson (Oculis S.A.) and Zoltán Fülöp encorporates a nice case study of preventing the oxidation of corticosteroids.

See the full patent on PatentScope


Improvement of Fertilization Capacity and Developmental Ability of Vitrified Bovine Oocytes by JUNO mRNA Microinjection and Cholesterol-Loaded Methyl-β-Cyclodextrin Treatment

Today's cyclodextrin,

This is a little reminder of the great potential to use these compounds (especially # cholesterol-loaded methyl-beta-cyclodextrin) to improve fertilization capacity. The fertilization and development ability of vitrified bovine oocytes were improved by the combination treatment of JUNO mRNA microinjection and CLC/MβCD – Chinese Academy of Agricultural Sciences

Read the full article here

Cyclo Therapeutics Announces First Patient Dosed in Phase 2b Study of Trappsol® Cyclo™ for the Treatment of Early Alzheimer’s Disease

carbohydrates, , , ,

Cyclo Therapeutics, Inc. announces first patient dosed in Phase 2b study of Trappsol® Cyclo™ for treating early Alzheimer’s disease.

Trappsol® Cyclo™ is the Company’s proprietary formulation of hydroxypropyl beta-cyclodextrin. In multiple clinical studies, it has shown encouraging results in effectively managing the transportation of cholesterol, a known defect in neurodegenerative diseases. Many known risk factors for Alzheimer’s disease are associated with cholesterol metabolism.

Cyclo Therapeutics is currently testing the same investigational Trappsol® Cyclo™ drug in Phase 3 clinical trial (TransportNPC™) and a long-term extension study for the treatment of Niemann-Pick disease Type C1, a rare, fatal, and progressive genetic disorder. Taking the place of the defective NPC1 protein, Trappsol® Cyclo™, with its cyclic structure, facilitates the transport of accumulated cholesterol out of cellular lysosomes so it can be further processed and excreted out of cells. With the biological similarities demonstrated between Niemann-Pick disease Type C1 and Alzheimer’s disease, including cholesterol accumulation in regions of the brain, elevated levels of Tau in cerebrospinal fluid (“CSF”), and amyloid plaques in the brain, the Company believes Trappsol® Cyclo™ has significant potential to be an effective treatment option for Alzheimer’s disease.

Read the full announcement here

ZyVersa Therapeutics Adds Two Esteemed Leaders in Nephrology to Its Renal Scientific Advisory Board to Support Clinical Advancement of Lead Renal Drug Candidate, VAR 200

carbohydrates, ,

ZyVersa Therapeutics Inc., developing, among others VAR200, a therapeutic 2-hydroxypropyl-beta-#cyclodextrin for FSGS, Alport syndrome, and diabetic kidney disease, just added two leading nephrologists to their Scientific Advisory Board.
We hope this will help move the program forward to follow this one-of-a-kind application of CDs with great excitement.

See the full article here