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Sulfamethoxazole:hydroxypropyl-β-cyclodextrin complex: preparation and characterization.

Claudia Garnero¹, Virginia Aiassa, Marcela Longhi

¹Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina.

Journal of Pharmaceutical and Biomedical Analysis

|February 25, 2012

Summary

This summary is machine-generated.

Hydroxypropyl-β-cyclodextrin (HP-β-CD) significantly enhances sulfamethoxazole (SMX) solubility and thermal stability through complexation. This study details the interactions and confirms complex formation in both solution and solid states.

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Area of Science:

Pharmaceutical Science
Physical Chemistry
Materials Science

Background:

Sulfamethoxazole (SMX) is an important antibiotic with limited aqueous solubility.
Cyclodextrins, like hydroxypropyl-β-cyclodextrin (HP-β-CD), are widely used to improve drug solubility and bioavailability.
Understanding drug-excipient interactions is crucial for developing effective drug delivery systems.

Purpose of the Study:

To develop and characterize a complex of sulfamethoxazole (SMX) and hydroxypropyl-β-cyclodextrin (HP-β-CD).
To investigate the interaction between SMX and HP-β-CD in aqueous solution and in the solid state.
To evaluate the impact of HP-β-CD on the solubility and thermal stability of SMX.

Main Methods:

Solubility studies to determine the complexation behavior in aqueous solution.
Fourier-transform infrared (FT-FTIR) spectroscopy and scanning electron microscopy (SEM) for solid-state characterization.
Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) to assess thermal properties.

Main Results:

Complexation with HP-β-CD significantly increased SMX solubility, exhibiting an A(N) type solubility isotherm.
A 1:1 complex stability constant of 302 ± 3 M⁻¹ was calculated.
FTIR, SEM, DSC, and TGA confirmed complex formation in the solid state and enhanced thermal stability of SMX.

Conclusions:

HP-β-CD effectively forms a complex with SMX, leading to improved solubility.
The developed SMX-HP-β-CD complex exhibits enhanced thermal stability.
This complexation strategy holds promise for improving the formulation and delivery of sulfamethoxazole.