Preparation of amino acid derivative aggregates and their application as a drug carrier

Abstract

Amino acids, as the basic components of proteins, can cross the barrier of the digestive tract through oral administration and directly participate in human physiological activities. In this study, the amino acid derivative N-(benzyloxycarbonyl) -L-proline (Z-Pro) was selected to form aggregates as a carrier for the delivery of antioxidant drugs. And the composite system was developed by mixing Z-Pro, hydrophobic antioxidant drug and water, followed by heating. This process takes advantage of the hydrogen bonding between the amino acid derivative molecules and water molecules, as well as the hydrophobic interaction between the side chains of the amino acid derivatives and the drug, and converts the amino acid aggregates into oral liquid formulations based on a liquid-liquid phase separation mechanism. These oral liquid formulations significantly enhance the solubility of hydrophobic antioxidant drugs, exhibit suitable viscosity and fluidity, and demonstrate good stability in a simulated gastrointestinal biological environment. The stability of this formulation was further confirmed by exploring the retention of antioxidant properties of the drug. This drug delivery system improves the efficacy of hydrophobic antioxidant drugs and offers great potential for anti-aging therapeutic strategies.