Formulation and optimization of pH-sensitive nanocrystals for improved oral delivery

LOPEZ-VIDAL, LUCÍA; PARODI, PEDRO; ACTIS, MARIBEL ROMANELA; CAMACHO, NAHUEL; REAL, DANIEL ANDRÉS; PAREDES, ALEJANDRO J.; IRAZOQUI, FERNANDO JOSÉ; REAL, JUAN PABLO; PALMA, SANTIAGO DANIEL

Drug Delivery and Translational Research

Springer

Año: 2023

2190-393X

he challenge of low water solubility in pharmaceutical science profoundly impacts drug absorption and therapeutic effectiveness. Nanocrystals (NC), consisting of drug molecules and stabilizing agents, offer a promising solution to enhance solubility and control release rates. In the pharmaceutical industry, top-down techniques are favored for their flexibility and cost-effectiveness. However, increased solubility can lead to premature drug dissolution in the stomach, which is problematic due to the acidic pH or enzymes. Researchers are exploring encapsulating agents that facilitate drug release at customized pH levels as a valuable strategy to address this. This study employed wet milling and spray drying techniques to create encapsulated NC for delivering the drug to the intestinal tract using the model drug ivermectin (IVM). Nanosuspensions (NS) were efficiently produced within 2 h using NanoDisp®, with a particle size of 198.4 ± 0.6 nm and a low polydispersity index (PDI) of 0.184,