Drug Development & Delivery: Bioavailability & Solubility – The Promise of Novel Ingredients

In a recent article with Drug Development & Delivery, Abzena’s Head of Formulation, Dr. Gary Watts discusses how novel excipients may be the answer to improving solubility challenges faced by formulators for many years.

In 2023, the Office of New Drugs and the Center for Drug Evaluation and Research (CDER) launched a voluntary Pilot Program for the Review of Innovation and Modernization of Excipients (PRIME). This program is intended to allow biopharmaceutical manufacturers to obtain FDA review of novel excipients. The development of novel excipients is gaining momentum as pharmaceutical companies seek improved performance and versatility in drug formulations. Novel substances support nanoparticle drug delivery for oncological medications to provide better stability and adoption of medicines.

Here is what Dr. Watts had to say on the promise of novel ingredients…

Formulating complex biologics, such as monoclonal antibodies (mAbs), fusion proteins, and bispecifics, require robust development strategies that are flexible and phase-appropriate in order to opti­mize them for solubility, delivery, safety, and sustained stability. Utilizing pre-formu­lation assessments to establish and char­acterize the physiochemical characteristics of the biologic can dictate which ap­proaches are taken during formulation de­velopment and allow developers to rapidly identify and solve any complex problems earlier on in the process, avoiding costly downstream issues.

In a recent case study, a customer of Abzena’s had acquired a novel mAb that had been formulated by another CDMO. However, there was an issue with the se­lected formulation due to the fundamental properties of the mAb not being assessed during pre-formulation. During refrigerated storage, the formulation exhibited signs of phase separation and gelation that were resolved by warming to room tempera­ture, without any apparent impact on quality, explains Dr. Gary Watts, Head of Formulation, Abzena.

“This was not ideal from a regulatory perspective or for patient administration,” he says. “A study was designed to evaluate the fundamental factors crucial to formu­lation stability, such as the optimum pH, and stability at high or low ionic strength.”

Dr. Watts says an optimal formulation was identified that showed the desired physical and chemical stability, and was clear, colorless and free of visible particles after >6 months storage at 2-8°C. Fur­thermore, solubility was sufficiently im­proved to allow the concentration.

Read the article in full here

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