A potential new delivery format for children and other people with swallowing difficulties is closing in on the clinic. Researchers at Brigham and Women’s Hospital and the Massachusetts Institute of Technology (MIT) have developed the technology to address the need for cheap, temperature-stable formats for the delivery of both water-soluble and insoluble molecules.
Alternatives to tablets already exist. Solutions and syrups are options for water-soluble drugs. However, as many molecules are insoluble in water, researchers have also developed suspensions. The problem is suspensions require the caregiver to shake the formulation to ensure accurate dosing. Recognizing the limitations of current delivery routes, researchers at Brigham and Women’s Hospital and MIT set out to develop a better option.
“Most liquid or semi-solid systems are water-based and pose limitations for delivering drugs that cannot be dissolved in water,” Ameya Kirtane, Ph.D., lead author of the paper, said in a statement. “Our system is an oil-based system gel, which makes it compatible with most drugs. This enables the formulation of drugs that were not available in semi-solid or liquid dosage forms and allows patients, especially children, to more easily take their medicine.”
To make the oral formulations, which the researchers call oleogels, gelling agents are used to adjust the consistency of cooking oils to stiffnesses ranging from thickened drinks to yogurt puddings. Surfactants are used to dissolve drug molecules at high concentrations.
The researchers ran a proof-of-concept study in pigs, providing early validation of the use of the system to deliver three water-insoluble anti-infectives—azithromycin, praziquantel and lumefantrine—as well as one water-soluble molecule, moxifloxacin. To deliver moxifloxacin, the researchers suspended the drug, thereby opening up the platform to use with hydrophilic molecules.
Having generated proof-of-concept data, the researchers enlisted trained tasters to assess the texture and flavor of the gel formulations. The panel tested formulations made with a range of oils and gelling agents to determine whether consumers are likely to accept them, leading to the identification of a set of potentially viable combinations.
With the researchers also assessing the ability of people to dispense the formulations from single and multidose containers, the team has evidence to support the initiation of a clinical trial. A first-in-human clinical trial to evaluate the delivery of azithromycin in an oleogel in healthy volunteers is in the works.