Novel Cocrystals of Dexamethasone

Overview

Dexamethasone exhibits therapeutic efficacies against various inflammatory conditions, including asthma, chronic obstructive pulmonary disease, and COVID-19. Its poor aqueous solubility however renders the bioavailability suboptimal. This invention showcases the rational design and characterization of hidden dexamethasone cocrystals possessing improved pharmaceutical properties, with an ultimate goal to facilitate an advanced drug delivery of a class of corticosteroids to benefit patients.

Technical name of innovation

Thermally activated cocrystallization of corticosteroids

Commercialisation opportunities

Co-development, technology licensing

Problem addressed

In attempt to salvage the clinical use of dexamethasone, this invention applies cocrystal engineering as a promising formulation technique for improving its pharmaceutical properties, including solubility and dissolution rate. The elusiveness of the dexamethasone cocrystal system was untangled by treatment of high temperature annealing, which functioned as an "on-off" control for the cocrystallization, coined "thermally activated cocrystallization".

Innovation

By cocrystallizing with highly hydrophilic coformers, the dissolution performance of dexamethasone has substantially improved, without compromising the structural integrity and safety of the drug.
The dexamethasone cocrystal is suitable to be reformulated into different dosage forms for targeted delivery to respiratory tract, such as nasal or inhalable powders, to strike COVID-19/chronic lung diseases where it deals the most damage.
The first dexamethasone cocrystal being synthesized and characterized in the history of medicine.

Key impact

The reformulation of the lower-priced small-molecule drugs via cocrystallization, using dexamethasone as an example, not only improves their pharmaceutical properties, but also has a positive impact on patient access. This invention illustrates how modern crystal engineering can fulfill a paradigm of cost-effectiveness.
The screening method and know-how developed in this invention can facilitate the discovery of more modern drug-drug and drug-herb cocrystals, offering a new direction for personalized medicine against various diseases by leveraging the synergy of drug combinations.
The success of this invention can encourage the local pharmaceutical industry to adopt cocrystal engineering as a promising formulation strategy to develop better future medicine and extend the drug development lifecycle.

Application

Different classes of corticosteroid compounds

Patent

US Application No. 18/307,992
CN Application No. 202310597221.0

Advanced Biomedical Instrumentation Centre

Biomedical instrumentation plays a critical and increasing role, albeit invisible to most people, in the healthcare industry by enabling more accurate diagnoses, effective treatments, and earlier intervention and prevention capabilities. Advancing the development of cutting-edge medical devices, actuators and sensors requires collaboration among talented scientists, engineers and clinicians, as well as an environment that facilitates the commercialisation of research results into real-world applications that are accessible to a broader population.

The mission of the Advanced Biomedical Instrumentation Centre is to accelerate progress in translating advanced biomedical instrumentation from research and development into real-world healthcare solutions that benefit people in Hong Kong and around the world. The Centre aims to foster collaboration among top-notch engineers, scientists and clinicians in the US and Hong Kong to develop next-generation microfluidics and low-cost instrumentation technologies. It also takes advantage of Hong Kong’ s vibrant start-up community to commercialise the research work tailored for Asian patients.

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