Anyone who’s ever opened a bottle of antibiotics or other medication and lamented the fact that they had to swallow a massive horse pill has also wished pills were smaller. Chemical engineers at MIT have found a way to load more drug into a tablet, which could mean smaller and easier to swallow pills in the future. The scientists say that about 60 percent of the drugs on the market have hydrophobic molecules as their active ingredients.
Those molecules aren’t soluble in water and can be difficult to formulate into tablets because they have to be broken down into very small crystals to be absorbed by the human body. Chemical engineers at MIT have devised an easier process for incorporating hydrophobic drugs into tablets and other drug formulations, like capsules or thin films. The technique involves creating an emulsion of the drug and then crystallizing it.
The process allows a higher dose of the drug to be loaded per tablet. According to MIT researcher Liang-Hsun Chen, an MIT grad student and lead author of the study, this is critical because if the scientists can achieve high drug loading, smaller dosages can be delivered to achieve the same therapeutic results. Smaller pills could also improve patient compliance because small doses of the drug would be effective.
Researchers on the project devised a more efficient way to combine hydrophobic drugs with methylcellulose by forming an emulsion. Emulsions are mixtures of oil droplets suspended in water, similar to a mixture of oil and vinegar used to make dressing for solids. Researchers note when the droplets are on the scale of nanometers in diameter, the mixture is called a nanoemulsion.
The researchers then combined the oil phase with methylcellulose dissolved in water using ultrasonic sound waves to create nanoscale oil droplets. Once the emulsion was formed, the researchers transformed it into a gel by tripping the liquid into a heated water bath. The nano crystal-loaded particles can be crushed into a powder and compressed into tablets using standard drug manufacturing techniques.