Demystifying modified release drug delivery - Unlocking controlled release

CR formulations are becoming indispensable for managing chronic conditions like epilepsy, diabetes, hypertension, and pain, where the precise, sustained release of medication is essential. (1,2) Yet, the path to developing modern CR pharmaceuticals comes with challenges—especially in understanding functional excipients that meet increasingly complex delivery demands. 

In our latest article, our global modified release technical experts, Dr Simon Roberts, Pedro Andrade and Jovic Kuo, dive into the key factors shaping the future of CR formulations.  

SR: With ageing populations and patients having chronic conditions that require regular medication, we need simple dosage forms that are designed with the patient in mind. Both age and simplicity of use have created growth in modified release products. You see, taking medication once a day to treat a chronic condition increases compliance and health compared to multiple tablets throughout the day. This also provides better results for the patient. 

JC: Modified release formulations can provide stable drug release, reducing the frequency of medication intake and leading to better adherence for patients. This is especially beneficial for chronic disease patients (such as those with hypertension, diabetes, and hyperlipidemia), and they tend to have fewer adverse reactions to MR drugs.  

SR: The greatest challenge is to design a robust, reliable dosage form that will deliver the correct dose at the correct time, every time. Variability in release profiles needs to be minimised within a batch and between different batches. Another challenge comes in loading the required amount of active pharmaceutical ingredients into a small, swallowable dosage form, whilst also having space for the other excipients required to deliver the active in the required manner. 

JC: High technical capabilities and advanced equipment are required to produce high-quality, controlled release formulations, leading to higher costs. Additionally, patient acceptance poses a challenge for modified release formulations; for instance, switching from taking medication three times a day to once a day can be a significant adjustment. Various points need to be considered, starting with patient education and implementing cost-effective production methods such as process optimization and bulk purchasing of raw materials. Thus, modified release formulations can help reduce overall production costs without compromising quality. 

 

PA: We can provide high-quality excipients to formulators with deep understanding and expertise in the properties and use in modified release formulations. These excipients are manufactured to tight, consistent specifications which provide excellent performance every time. Slight changes in polymer viscosity can lead to very different release profile, and we work with reliable and global suppliers that understand that chemistry. Additionally, being API providers as well, we have a deep understanding of the API characteristics where solubility and permeability deeply affect APIs release from the swollen hydrogel. We can also offer solutions that take advantage of synergies between different MR chemistries to develop formulations capable of delivering higher drug loadings in smaller tablets with the required modified release profiles. Understanding the influences of particle size, viscosity, as well as the hydration and dissolution characteristics of polymeric excipients is paramount to optimising CR formulations.  

In summary, functional polymeric excipients are essential for the effective formulation of controlled-release (CR) dosage forms. Leveraging advances in excipient technology allows pharmaceutical manufacturers to address the complexities of CR formulations, providing innovative solutions that align with the evolving demands of healthcare.