A composition for activating plant’s natural defense mechanisms to extend the shelf life and methods thereof

Today's cyclodextrin, ,

The agricultural use of CDs is often neglected, so here is an excellent example of exploiting their potential in this field. This includes the application of the encapsulated powder of the active ingredient, which is released in a sustained manner near the farm/agricultural produce. When the volatile active ingredient is released, it slows down the ethylene biosynthesis pathway and restricts microbial growth of fresh produce without any expensive technologies (refrigeration) and harmful chemicals (toxic). It can be adopted to any stage of the fruits and vegetable supply chain.

See the full patent on Patentscope

First-in-Class Small Molecule Drug Approvals of 2022

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First-in-Class Small Molecule Drug Approvals of 2022
Great collection by Drug Hunter.

Of the 36 novel small-molecule and large-molecule drugs approved by the FDA in 2022, 18 were first-in-class approvals, including 9 small molecules (excluding atoms).

Some of the notable small molecule first-in-class approvals of 2022 include:
Sunlenca (lenacapavir): the first approved drug targeting HIV-1 capsid, indicated for multi-drug resistant HIV with an impressive bi-annual dosing regimen (Gilead Sciences)

Sotyktu (deucravacitinib): the first approved de novo deuterated drug – an oral, allosteric tyrosine kinase 2 (TYK2) inhibitor for moderate-to-severe plaque psoriasis (Bristol Myers Squibb)

Ztalmy (ganaxolone): the first neurosteroid to be studied for epilepsy, approved for treating seizures in cyclin-dependent kinase-like 5 deficiency disorder, an oral GABA-A receptor modulator (Marinus Pharma) – a cyclodextrin-enabled formulation

Pyrukynd (mitapivat): the first approved therapeutic for pyruvate kinase (PK) deficiency – an oral pyruvate kinase activator that improves hemolytic anemia (Agios Pharmaceuticals)

Voquezna (vonoprazan): the first potassium-competitive acid blocker that acts via reversible potassium-competitive ion binding, approved for Helicobacter pylori infection (Phathom Pharmaceuticals)

See the full article here.

Passive, active and endogenous organ-targeted lipid and polymer nanoparticles for delivery of genetic drugs

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As fellow stakeholders in developing novel drug delivery in gene therapy, we greatly admire the review of Sean Dilliard and Daniel Siegwart from The University of Texas Southwestern Medical School describing passive, active and endogenous organ-targeted lipid and polymer nanoparticles. Amazing compilation!

See the full article here

Compositions and methods of promoting cellular hydration 

Today's cyclodextrin, ,

According to this patent from Eastpond Labs, a CD-containing beverage could improve the cellular hydration efficiency of our drinks. Moreover, the beverage composition could increase the lifespan in the multicellular organism.
Rather ambitious and very exciting. I cannot wait to see some data on more complex beings than C elegans.
What is your opinion? Could this actually work on humans?

See the full patent on Espacenet

First Genegut meeting and Ireland/UK visits

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Last week our CSO, Milo Malanga, had the privilege to attend the kick-off meeting of the GENEGUT consortia (a highly specialized, Horizon Europe team developing novel tools for the oral delivery of RNA to treat Crohn’s disease in Cork.

He also met the team of Mary McNamara (https://www.tudublin.ie/research/postgraduate-research/graduate-research-school/meet-the-team/marymcnamara.html) at Technological University Dublin to discuss expanding potential collaborations and visited the Astrazeneca site in Cambridge, UK.

We are grateful for all of your hospitality and look forward to developing fruitful relationships in 2023. 

Use cyclodextrins as a radiostabilizer

drug delivery, Today's cyclodextrin, , ,

Using CDs to stabilize drugs chemically is rather frequently used. But did you know that they can also be used to stabilize radiopharmaceuticals? According to the patent of GE HealthCare (Kristine Opsvik Wikene; Kahn Imtiaz Ahmed; Graeme McRobbie) combined with a radiostabilizer (like ascorbic acid), a cyclodextrin as co-stabilizer improves the stability of radiopharmaceuticals compared to using a conventional stabilizer.

See the full patent on Espacenet.



Synergistic Antitumor Potency of a Self-Assembling Cyclodextrin Nanoplex for the Co-Delivery of 5-Fluorouracil and Interleukin-2 in the Treatment of Colorectal Cancer

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We are proud to share Milo Malanga‘s most recent collaboration paper with Hacettepe University on creating nanoplexes via cationic cyclodextrin polymer, 5-Fluorouracil, and Interleukin-2 based on the opposite charge interaction of macromolecules without undergoing any structural changes or losing the biological activity of Interleukin-2. In the colorectal tumor-bearing animal model, survival rate, antitumor activity, metastasis, and immune response parameters were assessed using a cyclodextrin derivative, which was found to be safe based on the ALT/AST levels in healthy mice.

Histomorphometric analysis showed that the groups treated with the nanoplex formulation had significantly fewer initial tumors and lung foci when compared with the control. The dual drug-loaded nanoplex could be a promising drug delivery technique in the immunochemotherapy of colorectal cancer.

Safiye Akkın, Gamze Varan, Anıl Işık, Petek Korkusuz, Erem Bilensoy et al.

See the full article here

Direct cyclodextrin-based powder extrusion 3D printing of budesonide-loaded mini-tablets for the treatment of eosinophilic colitis in pediatric patients

Today's cyclodextrin, , ,

Have you ever wondered how cyclodextrins fit into modern, fancy formulation technologies like 3D printing? Nunzio Denora and his group at Università degli Studi di Bari and Institute of Crystallography – CNR show how to make budesonide-loaded mini-tablets using direct cyclodextrin-based powder extrusion 3D printing.

Monica Pistone, Giuseppe Francesco Racaniello, rosanna rizzi, Rosa Maria Iacobazzi, Ilaria Arduino, Antonio Lopalco, Angela Assunta Lopedota

See the full article here