Innovative Tablets Aim to Revolutionize Cancer Drug Delivery
Enzian Pharmaceutics, a startup co-founded by Aron Blaesi, PhD, and Nannaji Saka, ScD, is developing a novel oral tablet designed to deliver cancer medications more steadily over time. This innovative approach aims to address a common issue with traditional oral cancer drugs, which often dissolve rapidly in the stomach, leading to a sudden influx of medication into the bloodstream. Such quick release can result in side effects and limit the drug’s effectiveness as its concentration diminishes significantly after the initial dose.
Transforming Drug Release Dynamics
The tablets created by Enzian Pharmaceutics utilize advanced technology involving tiny 3D-printed fibers. These fibers transform into a gel-like substance upon contact with water, enabling the tablets to remain in the stomach for extended periods—up to a day in animal studies. As the gel degrades gradually, it releases the medication in a controlled manner.
Currently, the company is validating the ability of its tablets to remain in place within a small cohort of healthy human volunteers. Following this phase, Enzian plans to initiate trials to assess the technology’s effectiveness and safety for cancer patients within the next year. Blaesi emphasizes the potential benefits, stating, “A lot of orally delivered cancer drugs could benefit from this.” According to him, the high initial concentration of drugs can lead to severe side effects, while lower concentrations later in the dosing schedule may reduce therapeutic efficacy.
From Concept to Clinical Trials
After receiving his PhD from MIT in 2014, Blaesi aimed to apply his research to create a viable business. His early work at the Novartis-MIT Center for Continuous Manufacturing involved using injection molding to produce pills, a method that resulted in less porous tablets compared to traditional powder compaction. This insight led to a realization about the importance of tablet microstructure in drug release.
Blaesi and Saka shifted their focus from injection molding to 3D printing, allowing for greater precision in creating fibrous structures that could optimize drug delivery. The team experimented with various materials, discovering that those with higher molecular weights allowed for slower dissolution rates, which could be advantageous for sustaining drug availability in the stomach.
In 2019, Blaesi and Saka published their findings on expandable fibrous tablets for prolonged drug delivery, although the initial reception was mixed. Some experts expressed skepticism, suggesting that previous attempts to create similar formulations had failed. Undeterred, Blaesi conducted additional animal experiments during the COVID-19 pandemic, ultimately refining the tablet design to achieve the desired functionality.
The final tablet design incorporates a grid of tiny fibers that expand upon contact with gastric fluid, creating a robust gel that releases medication steadily. In animal studies, the team demonstrated that these tablets could remain in the stomach for between 12 to 24 hours, allowing for optimal drug absorption.
With an eye on human clinical trials, Enzian intends to test its tablets with a prostate cancer drug that is currently administered in doses of several hundred milligrams per day. Blaesi aims to reduce this dosage significantly while enhancing therapeutic outcomes. He believes that the technology could also be beneficial for treating various cancers, including those of the blood, skin, and breast.
As the startup prepares to transition into patient trials, the focus remains on maximizing treatment effectiveness while minimizing adverse effects. This crucial step is essential for demonstrating that their formulation can outperform existing therapies, as even a single adverse event could jeopardize the future of a new drug.
Blaesi reflects on the journey thus far, stating, “The opportunity is enormous. So many oral cancer drugs have this delivery problem.” With expectations set high for the upcoming trials, there is optimism that Enzian Pharmaceutics may indeed deliver on its promise of improving cancer treatment.
