Nanoparticles pave the way for biological drugs in tablet form
21 October 2022
In a new study, researchers at Uppsala University show how specially designed nanoparticles pave the way for oral delivery of biological drugs. "That the particles are absorbed in large quantities in the intestinal cells may facilitate medication for patients that have to inject their biological drug," says Patrik Lundquist, researcher in Drug Delivery.
Biological drugs, such as antibodies and other proteins, originate from living sources. They account for every third new medicine and their importance in modern healthcare is steadily increasing. However, their poor stability in the harsh environment of the gastrointestinal together with their large size that limits cellular uptake makes oral delivery difficult. Now researchers at Uppsala University present results that show that nanoparticles can increase local uptake of biological drugs in the intestine.
“In the European TRANS-INT research consortium, we have studied the fate of nanoparticles designed to deliver biological drugs by the oral route. Our research group has focused on the interaction between human intestinal tissue and the nanoparticles, and our observations show that the nanoparticles are absorbed in large quantities in the cells of the intestinal wall. This indicates that this method has potential to enable oral drug delivery to the intestine,” says Patrik Lundquist, researcher at the Department of Pharmacy.
The research at Uppsala University was conducted with human intestinal tissues donated by patients who underwent surgery at the Uppsala University Hospital. Thus, the research group managed to avoid animal studies, while also obtaining a more complete picture of how the nanoparticles behave in the human intestine.
“Several biological drugs break down before they reach the intestine when delivered orally. Those that do reach the intestine will, as a result of size and polarity, not be taken up by the target cell. Healthcare and patients therefore have to rely on injections. Our results demonstrate for the first time that specially designed nanoparticle formulations are taken up in large amounts by the cells in the intestinal wall. The finding was unexpected, since the original goal was to deliver biological drugs such as insulin to the patient’s circulation. Our collaborators at the University of Santiago de Compostela are now exploring if the nanoparticles can be used to treat intestinal disease instead, such as inflammatory bowel disease,” says Per Artursson, Professor of Dosage Form Design.
- In biological drugs, the active substance has been produced in or purified from material of biological origin such as living cells or tissue.
- Biological drugs enable more precise care and effective treatment of several major diseases.
- The nanoparticles in this study had a diameter of a few hundred nanometers. At this scale particles behave differently than particles of larger sizes and are attracting a lot of interest as drug delivery vehicles.
- Read article Barriers to the Intestinal Absorption of Four Insulin-Loaded Arginine-Rich Nanoparticles in Human and Rat (Lundquist P. et al., ACS Nano 2022)
- Research in Drug delivery at Uppsala University