Advancing Drug Delivery: Meeting the Challenges of Next-Gen Therapeutics

In the ever-evolving landscape of drug discovery, breakthroughs in molecular biology and genome sequencing are driving a surge of innovation in small and medium-sized modalities and targeted therapies. However, with progress comes challenges, particularly in delivering the next generation of small targeted therapeutics.

Despite remarkable advancements, a significant portion of disease-causing proteins remains untapped with current large molecule approaches. The quest for molecules blending the best attributes of small molecules and monoclonal antibodies has led to a paradigm shift towards druggability optimization. Enter proteolysis targeting chimeras (PROTACs), offering a catalytic approach to degrade pathogenic proteins previously deemed undruggable.

Yet, while PROTACs hold promise, their formulation presents hurdles. Residing in the chemical space beyond Lipinski’s Rule of Five, they exhibit challenging physicochemical properties like poor solubility and permeability. Additionally, their molecular flexibility adds complexity, necessitating innovative solutions for effective delivery.

Researchers have explored various technologies to overcome these challenges. From nano-sized carriers to nucleic acid-based systems, efforts abound to enhance solubility, stability, and site-specific accumulation of PROTACs. Examples include embedding PROTACs in amorphous solid dispersions, incorporating them into nanopolymeric micelles, and encapsulating them in polymeric nanoparticles conjugated with targeting ligands.

Among these approaches, mesoporous carriers like MesoPAC offer unique advantages. Engineered from FDA-approved cellulose derivatives, MesoPAC enhances drug dissolution and stability while enabling tunable release profiles. Its compactability into tablets ensures seamless translation to high-speed tableting machines, presenting a promising avenue for accelerating the development of novel therapeutic modalities.

As we navigate the frontier of drug delivery for next-gen therapeutics, selecting the right enabling technology is paramount. The formulation challenges ahead demand innovative solutions, and mesoporous carriers stand at the forefront, poised to transform the landscape of drug delivery and usher in a new era of targeted therapies.


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