Stabilization of cannabis resin and solid oral cannabinoid formulations

drug delivery, Today's cyclodextrin,

today’s cyclodextrin:
using CDs to solubilize and stabilize cannabinoids is very popular in the pharma and nutraceutical/food industries. The most recent paper I read on the topic is from Canntab Therapeutics, yet in the past 25 years, since the first paper from Pekka Jarho et al., we have seen cannabis seed oil stabilized by BCD, an herbal medicine pill for treating constipation, fructus cannabis pill for the treatment of constipation and bowel discomfort, tea for patients in gastric cancer, intestine-lubricating and bowel relaxing granules. Among foods, yogurt enriched with herbal excipients, such as cannabis seeds, and BCD as a health food is claimed useful for soothing nerves, reducing blood pressure and blood fat, dispelling wind-damp, cold, and heat, losing weight, resisting aging, and relaxing bowels. On the analogy of powdered alcohol (Palcohol) prepared by complexing alcoholic drinks with CD, powdered weed, the cyclodextrin-encapsulated cannabinoid is expected to get on the market. 

See the patent on Patentscope

Polysaccharide-based nanogels for biomedical applications: A comprehensive review

carbohydrates, drug delivery,

The biomedical, biotech, and food industries all use polysaccharides as vital biomolecules with a variety of applications. Polysaccharides have great potential as biomaterials, and polysaccharide-based nanogels have attracted a lot of attention as carriers for different bioactive agents due to their unique versatile groups, specifically for site-directed or controlled delivery of the payload and, particularly because of their physicochemical properties, biodegradability, and biocompatibility. The 3D polymer network of NG produced by chemical crosslinking or physical self-assembly may be used to incorporate hydrophilic or hydrophobic molecules, including tiny drugs and proteins, genetic material patterns, and even ultrasmall nanoparticles. In this review, the chemistry of specific common polysaccharides and the various methods used to fabricate polysaccharide-based NG is discussed, with an emphasis on their use NG as drug delivery systems.

FOUAD DAMIRI, Dr.Satish Rojekar, Yahya Bachra, Rajender Varma, Dr. Swetha Andra, Satheesh kumar Balu, Dr. Chandrakantsing Pardeshi, Vijaysing Pardeshi, Hitendra Patel, Ana Cláudia Paiva-Santos, Mohammed Berrada, Mónica Cristina García

See the full article here

Sialic acid-targeted cyclodextrin-based nanoparticles deliver CSF-1R siRNA and reprogram tumour-associated macrophages for immunotherapy of prostate cancer

drug delivery, drug development

Another important paper on cyclodextrin-assisted gene therapy from the GENEGUT consortium leader University College Cork (Caitriona O’Driscoll) now proposing a sialic acid-targeted cyclodextrin-based nanoparticle to specifically deliver CSF-1R siRNA to M2 macrophages. This targeted cyclodextrin-based siRNA drug delivery system provides a potential strategy for prostate cancer immunotherapy.
Monique Mendonça, Jianfeng Guo et al

See the article here

Three-in-one: exploration of co-encapsulation of cabazitaxel, bicalutamide and chlorin e6 in new mixed cyclodextrin-crosslinked polymers

drug delivery, ,

Another great paper comes out of the long-term collaboration between our CSO,Milo Malanga and Ilse Manet‘s lab at National Research Council of Italy.
We explored a series of cyclodextrin (CyD) polymers composed either of a single CyD type or a mixture of two CyD types to encapsulate simultaneously different compounds with potential therapeutic interest for multimodal prostate cancer treatment. Thanks to a single inexpensive CyD-based polymer, we produced a three-in-one platform for the future implementation of combined chemotherapy and photodynamic therapy. These achievements are most relevant as nanomedicines are continuously proposed, but their potential for translation to the pharma industry is compromised by their limited potential for industrial upscale.

Elisabetta Pancani, PharmD, Marco Agnes, Arianna Mazza, Alessandro Venturini et al.

See the full article here

Anomalous Properties of Cyclodextrins and Their Complexes in Aqueous Solutions

drug delivery, Today's cyclodextrin

today’s cyclodextrin:
This review by Thorsteinn Loftsson, Hakon Hrafn Sigurdsson, and Phatsawee Jansook pulls a brave topic. It accounts some of the unexpected results the authors have encountered during their studies of CDs as pharmaceutical excipients.
CDs are constantly surprising investigators with their unique physicochemical properties. CDs are solubilizing complexing agents of poorly soluble drugs in aqueous solutions, while they can also act as organic cosolvents like ethanol. CDs and their complexes self-assemble in aqueous solutions to form both nano- and microparticles. The nanoparticles have diameters that are well below the wavelength of visible light; thus, the solutions appear to be clear. However, the nanoparticles can result in erroneous conclusions and misinterpretations of experimental results. CDs can act as penetration enhancers, increasing drug permeation through lipophilic membranes, but they do so without affecting the membrane barrier.

See the full article here: Anomalous Properties of Cyclodextrins and Their Complexes in Aqueous Solutions


Grafting of Cyclodextrin to Theranostic Nanoparticles Improves Blood-Brain Barrier Model Crossing

drug delivery,

today’s cyclodextrin:
Core–shell superparamagnetic iron oxide nanoparticles hold great promise as a theranostic platform in biological systems. Antonino Puglisi and coworkers report the biological effect of multifunctional cyclodextrin-appended SPIONs (CySPION) in mutant Npc1-deficient CHO cells compared to their wild-type counterparts. CySPIONs show negligible cytotoxicity while they are strongly endocytosed and localized in the lysosomal compartment. Through their bespoke pH-sensitive chemistry, these nanoparticles release appended monomeric cyclodextrins to mobilize over-accumulated cholesterol and eject it outside the cells. CySPIONs show a high rate of transport across blood–brain barrier models, indicating their promise as a therapeutic approach for cholesterol-impaired diseases affecting the brain.

University of Natural Resources and Life Sciences, Vienna (BOKU): Peter van Oostrum, Erik Reimhult
Università degli Studi di Catania: Noemi Bognanni, Graziella Vecchio
Ege University: Ece Bayir
University of Oxford: Dawn Shepherd, Frances Platt

See the full article here: Grafting of Cyclodextrin to Theranostic Nanoparticles Improves Blood-Brain Barrier Model Crossing

Confocal micrographs of Npc1-deficient CHO after incubation with 0.1 mg/mL FITC-CySPION for 72 h showing co-localization, with Pearson’s coefficient of 0.37, between FITC-CySPION (green) and LysoTracker Deep Red within the lysosomal compartments (red) within the ROI preproduced on the right. The used excitation wavelengths and fluorescence maxima are indicated in the figures. The field of view is 290 × 290 µm2.

Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability

drug delivery

today’s cyclodextrin:
is about developing antisense oligonucleotide tablet formulations using high-speed electrospinning. Hydroxypropyl-beta-cyclodextrin (HPβCD) was used as a stabilizer and an electrospinning matrix from one of the best pharma groups in Hungary (FirePharma Research Group BME – Budapest University of Technology and Economics) collaborating with Janssen Inc.

The fibrous HPβCD–antisense oligonucleotide formulations showed no sign of physical or chemical degradation over the 1-year stability study, which also shows the suitability of the HPβCD matrix for the formulation of biopharmaceuticals. The obtained results demonstrate possible solutions for the challenges of electrospinning, such as scale-up and downstream processing of the fibers.

Edit Hirsch, Márió Nacsa, Edina Szabó, Panna Vass, Julia Domjan, Attila Farkas,Zsuzsanna Eke, Tamás Vigh, Sune Klint Andersen, Geert Verreck, György Marosi and Zsombor Kristof Nagy et al

See the full article here: Oligonucleotide Formulations Prepared by High-Speed Electrospinning: Maximizing Loading and Exploring Downstream Processability


An Engineered Nanosugar Enables Rapid and Sustained Glucose-Responsive Insulin Delivery in Diabetic Mice

carbohydrates, drug delivery

Glucose-responsive insulin-delivery platforms sensitive to dynamic glucose concentration fluctuations and providing both rapid and prolonged insulin release have great potential to control hyperglycemia and avoid hypoglycemia diabetes. RMIT University and Monash University present biodegradable and charge-switchable phytoglycogen nanoparticles capable of glucose-stimulated insulin release. The nanoparticles are “nanosugars” bearing glucose-sensitive phenylboronic acid groups and amine moieties that allow effective complexation with insulin (≈95% loading capacity) to form nano complexes. A single subcutaneous injection of nano complexes shows a rapid and efficient response to a glucose challenge in two distinct diabetic mouse models, this results in optimal blood glucose levels for up to 13 h. The nano complexes’ morphology is key to controlling rapid and extended glucose-regulated insulin delivery in vivo. These studies reveal that the injected nano complexes enabled efficient insulin release in the mouse, with optimal bioavailability, pharmacokinetics, and safety profiles. These results highlight a promising strategy for the development of a glucose-responsive insulin delivery system based on natural and biodegradable nano sugar.
Rong XU, Sukhvir Kaur Bhangu, Karly Sourris, Domitilla Vanni, Marc-Antoine Sani, Karen Alt, Be’eri Niego, Dr. Quinn A. Besford, Brendan Dyett, Irena (Iśka) Carmichael, Mark Cooper, Christoph Hagemeyer, Francesca Cavalieri, et al

See the full article here: An Engineered Nanosugar Enables Rapid and Sustained Glucose-Responsive Insulin Delivery in Diabetic Mice

Thiolated cyclodextrins: A comparative study of their mucoadhesive properties

drug delivery, Today's cyclodextrin

today’s cyclodextrin:
when it comes to CDs, mucoadhesive properties are rarely in focus. But why not?
Andreas Bernkop-Schnürch’s team at Leopold-Franzens Universität Innsbruck investigated the mucoadhesive properties of nonionic, negatively, and positively charged thiolated cyclodextrins (CDs), including α-, β-, and γ-CDs of the low and high degree of thiolation.
In conclusion, a high degree of thiolation and the introduction of cationic charges are mainly responsible for the high mucoadhesive properties of CDs and generate, GCD derivatives do better in this aspect.

See the full article here: Thiolated cyclodextrins: A comparative study of their mucoadhesive properties