Preparation and Release of pH-Sensitive β-Cyclodextrin Derivative Micelles Loaded with Paclitaxel

Area of Science:

• Polymer Chemistry
• Materials Science
• Nanotechnology

Background:

• Paclitaxel (PTX) is a vital chemotherapy drug with poor solubility.
• Developing effective drug delivery systems is crucial for improving PTX efficacy.
• Cyclodextrin-based copolymers offer potential for enhanced drug solubilization and targeted delivery.

Purpose of the Study:

• To synthesize and characterize a new amphiphilic copolymer, 6-β-CD-N-ODMA.
• To develop and optimize polymeric micelles as a drug carrier for paclitaxel (PTX).
• To evaluate the physicochemical properties, drug loading, and release kinetics of PTX-loaded micelles.

Main Methods:

• Synthesis of 6-β-CD-N-ODMA copolymer from β-cyclodextrin and octadecylamine.
• Preparation of paclitaxel (PTX)-loaded micelles using the dialysis method.
• Optimization of micelle preparation via orthogonal experiments.
• Characterization using fluorescence probe, FTIR, DLS, and SEM.
• In vitro drug release studies at different pH values.

Main Results:

• Successful synthesis of amphiphilic 6-β-CD-N-ODMA copolymer capable of forming polymeric micelles.
• Optimized drug-loaded micelles achieved a drug-loading content of 1.97%.
• Characterization confirmed the formation and properties of both blank and PTX-loaded micelles.
• The carrier demonstrated significant pH sensitivity, with 88% cumulative PTX release at pH 5.0 after 96 hours.
• PTX release kinetics at pH 5.0 best fit the Ritger-Peppas model, indicating hydrolysis as the primary release mechanism.

Conclusions:

• The novel 6-β-CD-N-ODMA copolymer effectively forms polymeric micelles for paclitaxel (PTX) delivery.
• The developed drug carrier enhances PTX solubility and exhibits pH-responsive release characteristics.
• These findings suggest the potential of this micellar system for improving the clinical efficacy of paclitaxel.