Rani Therapeutics, based in San Jose, USA, announced that RaniPill, a biomacromolecular delivery capsule developed by the company, demonstrated good safety and tolerability in its first human trial. The company plans to launch further clinical trials later this year to test the effects of RaniPill delivery drugs in humans. Perhaps the future of oral biologics is not far from us.

The idea of ​​converting an injectable dosage form into an oral dosage form is not novel, but research in this area has been slow due to the fact that biomacromolecules are usually hydrolyzed by enzymes in the gastrointestinal tract and they are not easily absorbed. The strategy adopted by Professor Lange and Rani is very similar. They are designed to help the absorption of biomacromolecules by designing a “micro-injector” in a capsule to inject the drug into the gastrointestinal tissue.

RaniPill's surface has an enteric coating that keeps the capsule from being dissolved by stomach acid as it passes through the stomach. When the capsule enters the intestine, the enteric coating dissolves because of a change in pH, while triggering a chemical reaction to swell a small balloon in the capsule. The expansion of the small balloon will generate enough pressure to inject the microneedle composed of the drug into the intestinal wall tissue to help the absorption of the drug. This capsule does not contain any metal, springs and any other ingredients that cannot be absorbed or expelled by the body. When the balloon completes the mission of shooting the microneedles, they will automatically deflate and drain from the body. And because there is no receptor in the intestine that feels sharp pain, the patient does not feel pain. Rani has conducted preclinical trials in pig and dog animal models for up to five years, successfully delivering more than 10 biomacromolecules, including antibodies, peptides and proteins.

In this human trial, volunteers took RaniPill without the drug. The test results showed that the volunteers did not feel the balloon inflation and the process of injecting the microneedles, and the residual part of the capsule could be successfully excluded. RaniPill showed good tolerance in both male and female volunteers. Moreover, the test results show that the capsules play a similar role in the intestinal tract, regardless of whether the volunteers are full or fast when taking the capsule. This means that food does not affect the function of the capsule.

“This unique innovation combines engineering, chemistry, materials science with anatomy, physiology and biochemistry to convert injectables into oral drugs,” said Rani Chairman and CEO Mir Imran. “RaniPill is the first The safety and tolerability demonstrated in human trials give us confidence that we will be preparing for human trials in the coming months to test the effects of capsule delivery drugs with octreotide, a drug used to treat acromegaly. "