Drug solubilization and delivery from cyclodextrin-Pluronic aggregates.

Area of Science:

• Materials Science
• Pharmaceutical Sciences
• Physical Chemistry

Background:

• Hydrophobic drugs often exhibit poor aqueous solubility, limiting their therapeutic efficacy.
• Pluronic F127 (PF127) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) are known excipients with potential for drug delivery applications.
• Understanding the complexation and behavior of PF127/HPbetaCD systems is crucial for developing effective drug formulations.

Purpose of the Study:

• To characterize colloidal systems of Pluronic F127 (PF127) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) for hydrophobic drug delivery.
• To investigate the complexation between PF127 and HPbetaCD and its impact on system properties.
• To evaluate the solubility enhancement and drug release characteristics of PF127/HPbetaCD systems for hydrophobic drugs like sertaconazole (SN).

Main Methods:

• Surface tension measurements to determine critical micellar concentration (CMC).
• 1H-NMR spectroscopy to confirm complexation and molecular interactions.
• Transmission electron microscopy (TEM) for morphological analysis.
• Solubility studies and in vitro drug release assays at physiological conditions.

Main Results:

• HPbetaCD addition increased the apparent CMC of PF127, indicating complexation via threading of HPbetaCD onto PF127 chains.
• HPbetaCD significantly raised the sol-gel transition temperature of PF127, enabling gelling at lower PF127 concentrations (13.4 mM).
• The PF127/HPbetaCD system demonstrated a 100-fold increase in sertaconazole (SN) solubility.
• Controlled, temperature-dependent drug release of SN was observed over one week at 37°C.

Conclusions:

• Complexation between PF127 and HPbetaCD enhances hydrophobic drug solubility and allows for tunable, controlled drug release.
• The developed PF127/HPbetaCD colloidal systems show significant potential as advanced drug delivery vehicles.
• These systems offer a promising strategy for improving the delivery and therapeutic outcomes of poorly soluble drugs.