Upon ingestion, the new Enzian dosage form resides in the stomach for several hours and steadily delivers drug into the blood. This enables enhanced effectiveness of many life-saving drug therapies.
ZURICH & CAMBRIDGE, Mass.–(BUSINESS WIRE)–At present, the effectiveness of oral therapies employing a sparingly water-soluble drug is often limited by the quantity of drug that can be delivered into the blood stream. Because the drug solubility is low, the drug dissolution rate in the gastrointestinal fluid and the drug absorption rate by the blood are inherently low, too. Moreover, because the gastric residence time of the prevalent capsules and tablets is short, the drug absorption time is short. Consequently, the bioavailability (i.e., the area under the curve of drug concentration in blood versus time) is too low.
To mitigate this limitation, Enzian Pharmaceutics has invented, and developed, a new dosage form comprising orderly arranged, drug-bearing fibers. Upon ingestion, the fibrous tablet expands due to water absorption and forms a gel-like substance that remains in the stomach for prolonged time. The gel-like substance steadily releases drug during its gastric residence.
The concept was validated by trials on dogs using the sparingly-soluble Leukemia drug nilotinib. The Enzian dosage form resided in the stomach for about six hours, and ensured a three-times greater bioavailability than the present drug particle-filled capsule. The results were published in the Royal Society of Chemistry Journal RSC Pharmaceutics [1,2].
According Dr. Aron Blaesi, Enzian’s founder and CEO, at present about 40% of approved oral-delivery drugs have compromised efficacy due to low bioavailability. The Enzian technology could be used to improve the effectiveness of many of these drugs. Moreover, Blaesi is not only thinking about marketed drugs: “I am particularly thinking about salvaging drugs that have never made it to market because of poor bioavailability,” he says. He adds: “By increasing the quantity of drug delivered, we might make many of them viable for oral therapy. This might enable bringing new drugs and new therapies to market that have so far been neglected, but with the right delivery technology could be far superior to the state of the art.”
Now Enzian is validating the fibrous dosage form on a small number of healthy human volunteers.
References
[1] A.H. Blaesi, H. Richter, N. Saka, Enhancing the bioavailability of sparingly-soluble drugs by expandable, solid-solution fibrous dosage forms, RSC Pharmaceutics, 2026, 3, 88-102. https://doi.org/10.1039/D5PM00195A
[2] RSC Pharmaceutics, 2026, 3, 265-266. https://doi.org/10.1039/D6PM90004F
About Enzian Pharmaceutics
Enzian Pharmaceutics has emerged from the doctoral thesis of Aron H. Blaesi at the Massachusetts Institute of Technology (MIT). It was founded by Dr. Blaesi counseled by Dr. Nannaji Saka, also an MIT alumnus. Enzian develops new oral solid dosage forms for improving the effectiveness and reducing side effects of drug therapies.
Contacts
Aron H. Blaesi, Ph.D.
[email protected]
www.enzianpharma.com
