Uncover 3 proven strategies to enhance patient compliance with ethylcellulose

Patient compliance is a pervasive challenge in modern day medicine, contributing to as much as 50% of treatment failures in the United States, as well as 125,000 deaths and up to 25% of hospitalizations every year.[i] Addressing this issue is crucial for improving health outcomes and quality-of-life for patients worldwide. While many factors contribute to non-compliance—from bitter-tasting active pharmaceutical ingredients (APIs) to difficulties with swallowing medications (dysphagia) and complicated dosing regimens—innovative formulation strategies can make a difference. For example, controlled release formulations can reduce the number of times a patient needs to take a medication, improving compliance long term. However, the success of controlled release and other techniques hinges on the performance of excipients like ethylcellulose.

In this article, we take a closer look at three ways formulators can leverage the benefits of ethylcelluloseexcipients, like ETHOCEL™ and Aquacoat^® ECD30, to transform treatment outcomes and patient experiences, and ultimately boost patient compliance. Read on to uncover how ethylcellulosecan be used as a taste-masking agent, as part of innovative disintegrating oral dosage forms and for controlled release drug delivery.

1. Enhance palatability to boost patient acceptance

Implementing strategic taste-masking techniques to conceal the bitter or unpleasant taste of a drug can significantly improve medication acceptance for many patients. There are many simple solutions to modify the perception of unpleasant taste, such as flavoring agents, sweeteners, or bitterness inhibitors.[ii] However, highly unpalatable drugs, like rupatadine fumarate (antihistamine) and paracetamol (non-opioid analgesic), require a more sophisticated approach.[iii]^,[iv] One proven method involves using excipients to physically prevent direct contact between a bitter API and taste receptors on the patient’s tongue.² The hydrophobic nature of ethylcellulose has made it the go-to excipientfor improving palatability in tablet formulations and other oral dosage forms. So, how does it work?

Ethylcelluloseexcipients do not dissolve on contact with saliva. Instead, they form a barrier membrane around the formulation, which encloses the bitter API taste, preventing it from being released. As a result, the bitter APIs don’t come into contact with the taste receptors on the tongue. Once the formulation reaches the stomach, the active ingredient is released from the barrier membrane through pores or rupture of the film, depending on the dosage format used. This technique makes drugs more acceptable to patients—a crucial factor for supporting long-term compliance.

1. Overcome swallowing challenges with unique disintegrating dosage forms

Some patients have difficulty swallowing oral medicines, a condition known as dysphagia. There are many reasons why a patient may have this condition, from neurodevelopmental delay to gastroesophageal reflux disease.[v] Dysphagia significantly compromises compliance because it directly interferes with a patient’s ability to take oral medications—the most common form of drug delivery. One way drug developers can help patients overcome barriers related to dysphagia is through unique orally disintegrating formulations, such as orally disintegrating tablets (ODTs) and orally disintegrating films (ODFs). These formulations are designed to rapidly disintegrate in the mouth without the need for water, making them easier to administer, especially for patients who struggle with swallowing traditional tablets.[vi]

Excipients are essential for enabling the unique properties of orally disintegrating formulations, each serving a distinct purpose. For instance, croscarmellose, commercially known as Ac-Di-Sol^®, acts as a superdisintegrant, promoting rapid disintegration upon contact with saliva, while mannitol provides excellent compactability and robust physical properties.[vii] Ethylcellulose, on the other hand, provides mechanical strength, stability and taste-masking properties in orally disintegrating formulations.[viii] Its ability to hide the unpleasant taste of bitter APIs is particularly important though, as ODTs and ODFs [ST2][RC3] remain in the oral cavity for longer periods of time compared to standard tablets.

In addition, granule formulations can provide a solution for patients who have difficulty swallowing tablets. Effervescent granules can be packaged into sachets that can be mixed with water by the patient for easier administration. Similarly to orally disintegrating dosage forms, ethylcellulose provides structural support and taste-masking properties in granule formulations too.

1. Optimize dosing with controlled release formulations

Controlled release formulations allow drug manufacturers to modulate the pharmacokinetic profile of an API, leading to more predictable, consistent and sustained drug levels in the bloodstream over time.[ix]Prolonging drug releasemeans patients may not need to take their medicine as often to reap the benefits, which has the potential to reduce dosing frequency and improve compliance.⁹Moreover, these specialized delivery systems can help to minimize drug level fluctuations, mitigating the risk of adverse reactions.

Functional excipients are key to modulating the release kinetics of APIs in these formulations, with factors like excipient chemistry, particle size and molecular weight all influencing controlled release performance.[x]^,[xi]Ethylcelluloseexcipients can be used to enable controlled release in hydrophobic matrix tablets—the most widely used controlled release format. Globally accepted by formulators and regulators, hydrophobic matrix tablets offer benefits such as an excellent safety record, modifiable release rates, and reproducible release profiles. Ethylcelluloseis used to form controlled release matrices and coatings.

When coated over a matrix or multi-particulate, ethylcellulose works by forming a non-water-soluble film, through which the API release is controlled by formation of porous pathways. Research from IFF Pharma Solutions reveals that increasing the coating thickness of ethylcellulose slows the drug release rate, as the drug has a physically longer path to diffuse across. Ethylcellulosealso supports controlled release in other dosage forms, such as multiparticulates and granules which can be adapted into patient-friendly formats like ODTs, ODFs, [LL4] liquids, and sachets.

Elevate patient compliance with industry-leading ethylcellulose polymers

Proven time after time, IFF Pharma Solutions offers a range of ethylcellulose excipients for different application requirements. Launched over 75 years ago, ETHOCEL™ was the first commercially available ethylcellulose excipient brand, and it remains a preferred choice for formulators today. It is available in a range of viscosity grades including fine powder grades which can be compressed to form hydrophobic matrix tablets for controlled release. ETHOCEL™ is also effective as a coating in organic-solvent based systems or dry-powder coating processes, providing excellent barriers for taste-masking and/or controlled release.

Moreover, IFF Pharma Solutions offers Aquacoat^® ECD 30, an aqueous dispersion of ethylcellulose. This solution enables drug diffusion across water-insoluble membranes, making it ideal for sustained-release barrier coatings, slow-release pharmaceutical coatings, moisture barriers, as well as taste-masking applications.

Ready to harness the potential of ethylcellulose excipients to boost patient compliance? Download our ETHOCEL™ brochure now.

[i] Medication Adherence: The Elephant in the Room. Medication Management. January 2018. Available at: Medication Adherence: The Elephant in the Room (uspharmacist.com)

[ii] Taste Masking 101: Optimize Taste And Improve Patient Outcomes. Webinar hosted by IFF and Adare Pharma Solutions. June 2021. Available at: Taste Masking 101 Optimize Taste And Improve Patient Outcomes (outsourcedpharma.com)

[iii] Wasilewska, K., Szekalska, M., Ciosek-Skibinska, P., Lenik, J., Basa, A., Jacyna, J., Markuszewski, M., & Winnicka, K. Ethylcellulose in Organic Solution or Aqueous Dispersion Form in Designing Taste-Masked Microparticles by the Spray Drying Tethylcellulosehnique with a Model Bitter Drug: Rupatadine Fumarate. Polymers. (2019) 11(3), 522.

[iv] Alhamidi R, Ibrahim W. Preparation and Evaluation of Taste Masked Paracetamol Microcapsules Research. Journal of Pharmacy and Tethylcellulosehnology. (2022).

[v] Roden, D. F., & Altman, K. W. Causes of Dysphagia Among Different Age Groups: A Systematic Review of the Literature. Otolaryngologic Clinics of North America. (2013) 46(6), 965-987.

[vi] Hannan PA, Khan JA, Khan A, Safiullah S. Oral Dispersible System: A New Approach in Drug Delivery System. Indian J Pharm Sci. (2016) 78(1):2-7.

[vii] Ghourichay MP, Kiaie SH, Nokhodchi A, Javadzadeh Y. Formulation and Quality Control of Orally Disintegrating Tablets (ODTs): Rethylcelluloseent Advances and Perspethylcellulosetives. Biomed Res Int. (2021) 24:6618934.

[viii] Okuda Y, Irisawa Y, Okimoto K, Osawa T, Yamashita S. Further improvement of orally disintegrating tablets using micronized ethylcellulose. Int J Pharm. (2012) 423(2):351-359.

[ix] Adepu S, Ramakrishna S. Controlled Drug Delivery Systems: Current Status and Future Direthylcellulosetions. Molethylcelluloseules. (2021) 29;26(19):5905.

[x] Paul Wan Sia Heng, Lai Wah Chan, Michael G Easterbrook, Xiaoman Li, Investigation of the influence of mean HPMC particle size and number of polymer particles on the release of aspirin from swellable hydrophilic matrix tablets, Journal of Controlled Release. (2001) 76:1–2, 39-49.

[xi] T.C. Dahl, T. Calderwood, A. Bormeth, K. Trimble, E. Piepmeier. Influence of physico-chemical properties of hydroxypropyl methylcellulose on naproxen release from sustained release matrix tablets. Journal of Controlled Release. (1990) 14:1, 1-10.