Scientists at Nanyang Technological University (NTU) in Singapore have developed a slow-release "micro-capsule" that floats in the stomach, deploying drugs throughout the day. Designed to help Parkinson’s patients strapped with hefty medication regimens, the micro-capsule could eventually be used to deliver drugs for diseases like diabetes, the team figures, and it's recently launched a startup to hustle its platform through the clinic.
Patients with Parkinson's disease often take multiple pills per day to keep their symptoms in check, so the NTU team set out to create a delivery platform that could cut down that dosing to just once—or at most, twice—daily, study lead and assistant professor at NTU’s School of Materials Science and Engineering, Joachim Loo, Ph.D., said.
Loo’s solution? “Floating micro-capsules,” loaded up with either a double or triple PD drug cocktail. The capsules successfully delivered a combination of levodopa, carbidopa and entacapone—sold by Novartis as the triplet Stalevo—over 24 hours in a mouse study published in the journal Small. What’s more, mice treated with the drug-loaded capsules had stable dopamine levels in the brain for that same amount of time, a sign that the capsule may produce fewer side effects than oral levodopa, Loo added.
Levodopa, a precursor to dopamine, is a gold standard Parkinson’s treatment used to help restore motor function—but as it stands, patients with advanced disease may need to take as many as six tablets per day, and they frequently experience “off” periods, when the drug’s effects wane before the next scheduled dose. Meanwhile, patients on higher doses of levodopa sometimes develop levodopa-induced dyskinesia (LID), resulting in uncontrollable, jerking movements.
Hence the need for a sustained-release delivery route, which could bolster patient compliance, curbing Parkinson’s symptoms and potentially negating the safety issues linked to higher treatment regimens in one fell swoop.
The micro-capsule is made of FDA-approved polymers, selected for their buoyancy as well as their ability to safely degrade in the body after delivering drug payloads, Loo said.
The polymer capsule can be paired with multiple drugs and “[floats] extremely well in the gastric region,” which prevents it from being flushed out into the small intestine—effectively using the stomach as a drug reservoir, Loo explained. The drug cargo then slowly diffuses through the gastric region while the leftover capsule is broken down into carbon dioxide and water.
Armed with promising animal and in-vitro data, the NTU team is wasting no time getting its micro-capsule into the clinic. It will also have the luxury of skipping phase 1 trials—unless preclinical testing produces any unexpected surprises—given that the drug cocktail paired with the capsule is already FDA-approved.
With NTU's support, Loo recently launched the startup LiberaTx, homing in on the Latin word for "release" to highlight his drug delivery ambitions. The startup’s first goal is to raise funds toward a phase 2a trial, which will most likely take place in Singapore, LiberaTx co-founder and CEO, Sashi Kesavapany, Ph.D., said in an interview—though the team is open to running tests in countries with larger patient pools like Australia, he said.
Once the company has wrapped its phase 2a, it will almost certainly look to run its phase 3 study abroad, Kesavapany said, floating Australia, Japan, Europe and the U.S. as possible locations. Those international late-stage tests align with the company’s goal to launch its Parkinson’s disease micro-capsule on as global a scale as possible, he added.
Meanwhile, the team has successfully paired its micro-capsule with antibiotics and thinks it could one day be used to help treat metabolic diseases such as diabetes, high cholesterol and high blood pressure, simplifying dosing across a suite of treatment fields.