Dibenzocyclooctyne linked lysine-cyclodextrin for efficient intranucleus delivery of proteins

Now, this is something we have never seen before. Delivering oligonucleotides into cells using cyclodextrin-based nanoparticles has been studied a lot, yet in the paper from Chongqing University, intranucleus delivery of proteins is shown. This will certainly open up new drug delivery possibilities for the future and trigger novel applications.

Read the full article on ScienceDirect

In Utero Enzyme-Replacement Therapy for Infantile-Onset Pompe’s Disease

Amazing therapeutic success led by UCSF Pediatrics joined by Duke UniversityOttawa University, and Washington University via in-utero enzyme-replacement therapy for infantile-onset Pompe’s disease: Patients with early-onset lysosomal storage diseases are ideal candidates for prenatal therapy because organ damage starts in utero. After receiving in-utero ERT and standard postnatal therapy, the current patient had normal cardiac and age-appropriate motor function postnatally, was meeting developmental milestones, had normal biomarker levels, and was feeding and growing well at 13 months of age.

See the full article here

New clinical trial upcoming using cyclodextrin as active

Cyclo Therapeutics, Inc. sponsors Phase II trial for early Alzheimer’s disease. The study will enroll approximately 90 male and female patients aged 50 to 80 years who will be given a minimum active dose of 500 mg/kg of Trappsol Cyclo (equivalent to 18,500 mg/m2) as an intravenous (IV) infusion once every 28 days for 6 months.
We wish the best of success to our colleagues at Cyclo Therapeutics and hope this therapy will prove useful for the benefit of these patients.
Having programs ourselves in developing NCEs for neurodegenerative diseases, we find this study particularly essential.

Read more about the clinical trial here

Prostate-specific membrane antigen (PSMA) ligands comprising an amylase cleavable linker

Using sugars in a prodrug concept is a fascinating idea as these compounds can bring so much to the table like improve stability, PK, or help in targeting. In this patent from Heidelberg University oligosaccharide conjugated prostate-specific membrane antigens are described where the bonds are cleaved by amylase in the body.

See the patent on espacenet

Cyclodextrin-based delivery systems in parenteral formulations: A critical update review

We truly believe in the potential cyclodextrin hold in drug delivery in traditional formulations and upcoming applications like protein and oligonucleotide delivery, controlled or targeted release, and nanotechnology. Of course, our research is closer to the latter applications.
In this review published by Universidade de Coimbra (Laura FerreiraJoana Campos, Francisco Veiga Catarina Cardoso, and Ana Cláudia Paiva-Santos), parenteral applications and their potential a summarized very well.
Great educative read! 

Design, Synthesis, and Characterization of Stapled Oligosaccharides

From peptides to sugars: Design, Synthesis, and Characterization of Stapled Oligosaccharides. Oligosaccharide stapling increases enzymatic stability and cell penetration, opening new opportunities for using glycans in medicinal chemistry. – Max Planck Institute Manuel Garcia RicardoEmelie Ellen Reuber, Ling Yao, José Angel Danglad-FloresMartina DelbiancoPeter Seeberger
Wonderful chemistry and insightful new possibilities.

See the full article here