pH-Sensitive drug delivery system based on hydrophobic modified konjac glucomannan

Area of Science:

• Biomaterials Science
• Drug Delivery
• Nanotechnology

Background:

• Konjac glucomannan (KGM) is a natural polysaccharide with biocompatible properties.
• Developing efficient intracellular drug delivery systems is crucial for effective cancer therapy.
• Stimuli-responsive materials offer enhanced control over drug release kinetics.

Purpose of the Study:

• To synthesize and characterize amphiphilic konjac glucomannan-grafted aliphatic amine (KGM-g-AH) micelles.
• To investigate the potential of these micelles for acid-triggered curcumin release.
• To evaluate the safety, biocompatibility, and cellular uptake of KGM-g-AH micelles for intracellular drug delivery.

Main Methods:

• Two-step synthesis utilizing Schiff's base formation for KGM modification.
• Preparation and characterization of KGM-g-AH micelles, including size and stability analysis.
• In vitro studies on curcumin loading, release kinetics, pH-responsiveness, cytotoxicity, and cellular uptake.

Main Results:

• KGM-g-AH micelles were successfully synthesized, with KGM-g-AH8 forming stable spherical nano-micelles (107.6±11.6nm).
• These micelles demonstrated high curcumin loading capacity and good physical stability over 28 days.
• In vitro studies confirmed controlled release, endosomal/lysosomal pH responsiveness, intracellular pH-sensitivity, safety, and biocompatibility.

Conclusions:

• KGM-based micelles are feasible and promising strategies for cancer therapy.
• The developed micelles offer new potential options for intracellular drug delivery.
• The Schiff's base linkage provides an effective "switch" for acid-triggered drug release.