pH-responsive amphiphilic macromolecular carrier for doxorubicin delivery:

In this work, pH-sensitive amphiphilic macromolecules are designed to possess good biocompatibility and drug loading while employing an acid-sensitive linkage to trigger drug release at tumor tissues. Specifically, two pH-sensitive amphiphilic macromolecules were synthesized with a hydrazone linkage between the hydrophobic and hydrophilic segments. The chemical structure, molecular weight, critical micelle concentration, micelle size, and pH-triggered cleavage of the amphiphilic macromolecules were characterized via matrix-assisted laser desorption/ionization time-of-flight, nuclear magnetic resonance, and dynamic light scattering techniques. Drug loading and release as well as cytotoxicity studies were performed using doxorubicin. Hydrodynamic diameters of the micelles formed with pH-sensitive amphiphilic macromolecules were within an optimal range for cellular uptake. The critical micelle concentration values were 10–8–10–6 M, indicating micellar stability upon dilution. The degradation products of the ...