Automating the process of screening excipients for solubilising drug candidates

8 Nov 2017

The process, which uses significantly less materials than the manual alternatives, will ultimately improve drug developers’ clinical pathway.

Drug development is often a lengthy process fraught with difficulties, which increase costs. Selecting the right excipient to improve a compound's solubility is one such hurdle. Amjad Alhalaweh, a research scientist at Recipharm’s development facility in Uppsala, Sweden, offers his insight and expertise on how drug developers can expedite the process of excipient selection.

Automating the process of screening excipients for solubilising drug candidates
Recipharm development.

Often excipients are added to compounds to improve their solubility and dissolution properties during the development process. Why is it important to solubilise compounds with low aqueous properties at this stage of drug development?

A large number of newly discovered molecules have properties which can make the drug development process more complicated. Despite their superior pharmacological properties, these drug molecules risk withdrawal from drug development because of properties such as poor aqueous solubility. During the early drug development phase, it is important to assess the pharmacological, pharmacokinetics and toxicological profile of a compound to determine its safety, quality and efficacy. To do this effectively, they must be tested in liquid formulations hence selecting the optimum excipients to solubilise different compounds is of vital importance.

How do drug developers currently select appropriate excipients to solubilise compounds and what are the challenges that drug developers face following current procedures?

Currently the most popular methods of selecting excipients to solubilise compounds are based on trial and error approaches, so testing excipients manually until they find one that works. Because of the timeframes associated with this method, drug developers risk missing the most appropriate excipient and incurring high costs in terms of human resource and raw materials.

Generally speaking, the process usually takes at least 3-4 weeks and demands a large amount of API to establish a robust formulation. This has always been a problem in drug development, but it has become more prominent in recent years as more complex molecules enter the drug pipeline.

Can the process of selecting excipients be automated?

In short, yes. Recent developments in technology and analytical techniques coupled with the nature of screening excipients mean the process lends itself well to being automated. By selecting a screening list of excipients with a diverse range of solubilisation mechanisms, for example, including non-ionic surfactants, organic liquids and cyclodextrins, it is possible to include enough variations to offer accurate and successful results. Added to this, technologies such as the Tecan automated dispenser are ideal for dispensing the compounds into well-plates prior to the shaking process.

With this in mind, scientists at Recipharm have developed an automated high-throughput screening (HTS) method capable of reducing the timeframe of selecting suitable excipients from 3 to 4 weeks, to 3 to 5 days. The method is now being offered as part of our drug development service.

How much compound is used in your HTS method and what kind of excipient do you use?

Our HTS method can be optimised based on how much material is available but generally speaking we can use this process with about 100-200 mg of raw material. We can use any generally recognised as safe (GRAS) excipients and use specific criteria when selecting which ones to screen, for example, based on the drug delivery system. This flexibility means the method can be optimised to suit specific project requirements.

What are the benefits of automating excipient selection during the drug development phase?

Automating the excipient selection process offers drug developers huge benefits in terms of establishing a robust formulation quickly while using significantly less materials than the manual alternatives. If successfully implemented, automating the process will ultimately improve drug developers’ clinical pathway.

Not only does this have obvious benefits in terms of getting compounds to trials more quickly, but it also saves costs relating to staff resource and raw materials. And, this will be invaluable as more complex molecules with solubility challenges continue to enter the drug pipeline over the next few years. Automating this element of the drug development cycle will help pharmaceutical companies to improve their formulation strategies and in the long-run take new therapeutics to market more efficiently.

Amjad Alhalaweh is responsible for developing solutions for complex formulation challenges for both newly discovered compounds and existing drugs, along with finding new, cost-effective approaches for formulation design. He has specific expertise in the development of liquid formulations through crystallisation, solid-state characterisation and solid form screening and selection. He also delivers lectures at Uppsala University on the formulation of poorly soluble compounds.

Read More

Related tags

Market News

Related news

Spanish CDMO working ahead of EU serialisation deadline

Spanish CDMO working ahead of EU serialisation deadline

6 Dec 2018

Company now able to serialise commercial batches manufactured by them for clients; it can also offer standalone serialisation services as an outsourcing partner.

Read more 
Fluidic Analytics raises $31m to launch new lab tools and unlock biology behind major diseases

Fluidic Analytics raises $31m to launch new lab tools and unlock biology behind major diseases

5 Dec 2018

The financing will power the global commercial launch of the company's Fluidity One system.

Read more 
OnDosis and Recipharm partner to advance a novel treatment regimen for ADHD

OnDosis and Recipharm partner to advance a novel treatment regimen for ADHD

4 Dec 2018

The new treatment will leverage OnDosis’ proprietary technology, which integrates oral drugs in form of micro units and individualised dosing, in a handheld device.

Read more 
India to have strongest global growth in 2019?

India to have strongest global growth in 2019?

4 Dec 2018

Main drivers cited as ‘high-growth domestic market’ and ‘expanding manufacturing exports’.

Read more 
Catalent to expand biologics packaging capabilities

Catalent to expand biologics packaging capabilities

3 Dec 2018

Company's $14 million investment follows twentieth commercial drug approval at Bloomington, Indiana site.

Read more 
Merck successfully divests Consumer Health

Merck successfully divests Consumer Health

2 Dec 2018

Closing of sale to Procter & Gamble at a cash purchase price of €3.4 billion completed.

Read more 
Digital manufacturing is a top priority for life sciences

Digital manufacturing is a top priority for life sciences

29 Nov 2018

Zenith Technology survey reveals that more than half of those surveyed believe that Industry 4.0 will drive the most change.

Read more 
NIH to evaluate effectiveness of male contraceptive skin gel

NIH to evaluate effectiveness of male contraceptive skin gel

28 Nov 2018

The gel formulation includes the progestin compound segesterone acetate, in combination with testosterone, and is applied to the back and shoulders and absorbed through the skin.

Read more 
QPS expands US-based Phase I clinical trial capabilities

QPS expands US-based Phase I clinical trial capabilities

27 Nov 2018

Expansion supports the growing needs of the company's pharmaceutical, biotechnology and CRO partners.

Read more 
Hikma announces injectable licensing agreement

Hikma announces injectable licensing agreement

27 Nov 2018

Company provided with exclusive rights to market a suite of Hansoh's injectable oncology medicines within the US for the next 5 years.

Read more