Smallest-ever Milled Ingredients Improve Drug Delivery
Researchers at the NSF-funded Engineering Research Center (ERC) for Structured Organic Particulate Systems (CSOPS) at Rutgers, The State University of New Jersey, have realized a pair of novel outcomes in the formation and stabilization of nanoscale active pharmaceutical ingredients (nano-APIs). First, the CSOPS team created the smallest ever milled APIs. Secondly, long-term stabilization of APIs was achieved without the use of surfactants.
Both of these advancements have direct implications for improving the quality of drugs. Milled APIs exhibit an inherent consistency that cannot be matched by alternative methods. By achieving such small sizes, drug delivery is greatly enhanced. The elimination of surfactants in the stabilization process increases the purity of the drug, while reducing or eliminating the adverse effects of using surfactants.
This project specifically targets the improvement of BCS (Biopharmaceutics Classification System) Class II drugs, which do not dissolve well and therefore make delivery to the body slow or difficult. The APIs created by CSOPS’s novel milling process had a median diameter (d50) of less than a hundred nanometers, the first of its kind. Surfactants are commonly used in drugs delivered as tablets. They stabilize and help maintain the integrity of the drug, but add impurities and require larger doses. This project showed that using superdisintegrants (SDIs), compounds that aid in dissolving drugs in the body, achieved delivery rates similar to that of conventional tablets. Furthermore, the finely milled APIs were in 20-micrometer edible films, similar to breath strips, and achieved delivery rates far faster than the nanocomposite micro-particles (NCMPs) either with or without surfactants.