2025 Summit on Innovations in Controlled Release, Bioavailability Enhanceme

Modified release (MR) drug delivery systems play a critical role in optimizing therapeutic outcomes, improving patient compliance, and extending product lifecycles. This presentation explores a comprehensive, science-driven approach to MR formulation development, integrating modern modeling tools, robust technology platforms, and strategic development methodologies.
The session will highlight the role of physiologically based pharmacokinetic (PBPK) modeling in assisting formulation design, enabling prediction of in vivo performance and supporting accelerated development with minimal pharmacokinetic study iterations. The use of biorelevant and predictive dissolution methods to establish in vitro-in vivo correlations (IVIVC) that reduce development time and risk will also be discussed.
A broad spectrum of modified release technologies will be discussed, including matrix-based systems (erodible and diffusion-controlled), multiparticulates, bilayer tablets, osmotic tablets, and controlled-release of amorphous solid dispersions.
Each technology will be evaluated in terms of its ability to meet specific pharmacokinetic profiles, align with the Quality Target Product Profile (QTPP), and fulfill therapeutic goals. The presentation will explore how to select the most cost-effective technology without compromising performance, guided by a Quality by Design (QbD) framework that ensures a scientifically sound and risk-managed development strategy.
Attendees will gain insight into rational technology selection, efficient formulation pathways, and how MR systems can be leveraged not only to improve patient outcomes but also to strategically position products throughout their lifecycle.

Pharmaceutical salts are a commonly used strategy to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The selected salt form is expected to have high solubility to obtain optimal supersaturation and sufficient physical stability for adequate shelf life. In this presentation, we aim to develop equations to describe critical parameters of salts, including pH-solubility profile and pH_max. The equations serve as a valuable tool to aid in the calculation of salt solubility at pH below the pH_max in the presence of common counter ions. This provides the knowledge to assess the risks of pre-selection of the salt formers without the necessity of salt synthesis. The solubilities calculated by this model demonstrate good agreement with experimental solubility results reported in the literature. Compared to the conventional approaches for salt solubility and pH_max calculation, our model stands out, especially for poorly water-soluble bases with low pK_a values, which benefit the most from salt formation. Moreover, the equations are used to support the concept that salt selection should focus on finding salt forms with sufficient solubility, rather than the most soluble salt, as excessively high solubility could be detrimental to physical stability.

With about 20 worldwide approvals and almost a decade of commercial applications, CM is fertile ground for the next generation of implementation. Progress in the next few years will be fueled by major competitive advantages of CM:
- The faster speed in development of new products and processes enabled by CM will make it a central technology in pharmaceutical reshoring.
- The greater ability to model and control CM processes and improve quality control provides a major opportunity for the implementation of advanced manufacturing methodologies aligning closely with the FDA AMT designation program, enabling faster review of NDAs, ANDAs, and PAS.
- New formulation methods for continuous direct compression enable major reductions in the effort and materials required to develop or transfer manufacturing processes

Led by Dr. James Scicolone, will tour the first pioneering full-scale continuous direct compression tablet manufacturing line. This line is spread across a 3-floor equipment train including excipient dispensing, continuous blending, and tablet compression, all monitored by advanced process analytical technology (PAT) for real time content uniformity and near-instant release testing.
This facility served as the prototype for Janssen Pharmaceuticals' continuous manufacturing line in Gurabo, Puerto Rico, developed in collaboration with Rutgers.
In 2016, the FDA approved this line for producing PREZISTA (darunavir), marking it as J&J’s first commercial product manufactured using continuous processes.
The transition to continuous manufacturing, supported by a myriad of pharmaceutical companies and FDA , helps to enhance efficiency, reduce waste, and accelerate time-to-market for medications .