Intellectual Property

Intellectual Property (IP) is an important element of any pharmaceutical development programme. It allows the value of a product to be realised, and enables sound investment into research and innovation.

Crystec are committed to supporting our clients in securing IP and maximising the life of their products. Where this is a direct driver, Crystec’s unique proprietary mSAS® technology can offer further opportunities for enhanced protection, providing distinct advantages through a range of IP strategies.

mSAS® strategies for enhanced intellectual property

A unique process

Crystec’s mSAS® (modified Supercritical Anti-Solvent) technology is a unique and proprietary platform developed by a dedicated team of experts with extensive experience in the fields of supercritical fluids and pharmaceutical development. Developed from the principle of exploiting the highly tuneable solubility properties of supercritical fluids (SCFs), and knowledge of a variety of supercritical fluid-based applications, mSAS® has been engineered to maximise versatility and scalability, to support the development and commercialisation of therapeutics across a range of molecule classes and dosage forms.

New solid-state forms

Polymorph screening plays an important role in establishing a robust IP position. Crystec’s mSAS® technology is a highly effective tool in isolating ‘known’ stable and metastable polymorphs, as well as in identifying polymorphic forms unique to the high-pressure SCF environment. As such, mSAS® is often used as an enhanced polymorph screening technique for both new chemical entities and currently marketed APIs. Please see our case study to find out more.

Scalable co-crystals

The motivation for exploring pharmaceutical co-crystals is similar to that of polymorphs, but offers the additional advantage of selecting a range of functional co-formers. Co-crystals provide opportunities for improved pharmaceutical properties (solubility, stability, delivery etc.), in addition to being a powerful source of IP. However, one of the major challenges of pharmaceutical co-crystals is the difficulty in identifying scalable manufacturing processes. mSAS® is a thermodynamically stable process, which provides an attractive, single-step and highly scalable approach to co-crystal manufacture. Furthermore, mSAS® can be used to separate closely related co-crystal forms, which can often prove challenging for conventional processes. Read our case study to find out more.

In-particle design® formulation

Formulation is an often complex process which aims to optimise therapeutic performance, but also underpins the IP position of many pharmaceutical products. Crystec’s mSAS® technology offers an innovative approach to drug formulation, allowing the generation of composite particles containing a uniform and precise ratio of agents (multiple APIs or API plus excipients) in each particle. The intimate mixture of constituents in mSAS® particles can often facilitate improved performance (potentially leading to reduced excipient loading), and can be achieved using a single-step manufacturing process with simultaneous control over a range of particle properties (e.g. particle size, shape, solid-state form). Overall, in-particle design® formulation can be used to both simplify formulations, and to support the development of innovative combination products.

Novel routes of delivery

Enabling alternative routes of delivery can be attractive for many reasons, from improving patient care through easier to use and pain-free products, reducing the burden on healthcare systems by facilitating treatment outside of clinical settings, and providing opportunities for new IP. This is particularly the case with injectable or intravenous dosage forms.  However, for many therapeutics, alternative routes of delivery can be prohibitive due to a variety of factors such as first pass metabolism, or the ability to achieve adequate systemic concentrations.

Inhalation offers an attractive route of administration, not only for the local treatment of respiratory diseases, but also for rapid systemic update in the treatment of a variety of conditions. Because mSAS® particles are precipitated directly from solution, they have smooth, low energy surfaces, good flow behaviour, and display strong aerodynamic performance characteristics. This, combined with the ability to tune a range of crucial properties such as particle size, make mSAS® particles particularly suited to targeted lung delivery. To learn more, please read our case study.

Protection through patents and know how

By building performance into particles, mSAS® enables the development of products that perform well in simple, off-the-shelf devices. As a result, the need for complex device development programmes can be eliminated, meaning inexpensive, non-IP encumbered inhalers can be used, while achieving optimal product performance.

Rapid development

mSAS® is a proprietary technology platform designed and operated through extensive know-how acquired over many combined decades dedicated to the advancement of particle engineering and pharmaceutical development. Crystec hold several patents for products developed using the mSAS® platform, and are committed to supporting our clients in securing enhanced IP protection.

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Improving Dissolution

40% of marketed drugs and up to 90% of those in development exhibit poor solubility1. mSAS® provides different ways to address this challenge, including through increasing surface area, reducing agglomeration, new solid-state forms, co-crystals or stabilised amorphous forms of drug molecules.

Optimised Inhaled Therapies

mSAS® enables the design of drug particles of precise size and shape, that aerosolise even in patients who may struggle to breathe. As well as treating lung disease, inhaled therapies can be designed to enter the bloodstream, providing opportunities for fast onset and an alternative to painful injections.

Enhancing Stability

Chemical and physical stability is vital to ensure that therapeutics can be manufactured, stored, transported and administered to patients without a loss of efficacy or safety. mSAS® enables manufacture of highly pure, residue-free drug particles, capable of resisting moisture, and able to withstand higher temperatures.

Simplified Formulations

Formulation is often a complex, multi-step process, adding considerable time and cost to development. The mSAS® process involves a single step, and enables design of particles which contain all the components required for a medicine to perform, reducing the need for downstream processing.

Biomolecule Processing

Biotherapeutics such as peptides, proateins, antibodies and oligonucleotides are often delicate and easily damaged. mSAS® provides a gentle way to process biomolecules as free-flowing powders, retaining high levels of activity, reducing cold chain and enabling easier reconstitution.

Natural Products

Natural products are often highly complex and conventional approaches to their extraction, purification and formulation can be inefficient and often result in a poor-quality product. mSAS® simplifies production of natural products, allowing fine tuning of the components of a medicine and improvements in quality and consistency.

Green Manufacturing

Improvements in human health should not come at the cost to the planet, yet traditional approaches to medicines manufacturing carry a high environmental burden. mSAS® enables the production of medicines with lower waste, reduced emissions, using less solvent, and greatly improved energy efficiency.

Intellectual Property

Innovation in medicines development often requires robust protection of intellectual property (IP). The mSAS® process provides numerous opportunities to enhance IP, whether through novel solid-state forms, improved formulations or new routes of delivery.