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Drug solubilization and delivery from cyclodextrin-Pluronic aggregates.

A I Rodriguez-Perez¹, C Rodriguez-Tenreiro, C Alvarez-Lorenzo

¹Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782-Santiago de Compostela, Spain.

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Summary

Pluronic F127 (PF127) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) form colloidal systems that enhance hydrophobic drug solubility and enable controlled release. This combination offers a promising drug delivery platform with tunable properties for extended therapeutic applications.

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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.