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Flutamide-hydroxypropy-beta-chiyclodextrin complex: formulation, physical characterization, and absorption studies

Z Zuo¹, G Kwon, B Stevenson

¹Faculty of Pharmacy & Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada.

Journal of Pharmacy & Pharmaceutical Sciences : a Publication of the Canadian Society for Pharmaceutical Sciences, Societe Canadienne Des Sciences Pharmaceutiques

|September 20, 2000

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This study shows that hydroxypropyl-beta-cyclodextrin (HPbetaCyD) significantly enhances flutamide (FLT) solubility. However, HPbetaCyD decreases FLT transcellular permeation in Caco-2 cell models, except at high dilutions.

Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems
Biopharmaceutics

Background:

Flutamide (FLT) is an anti-androgen drug with poor water solubility.
Hydroxypropyl-beta-cyclodextrin (HPbetaCyD) is a common excipient used to improve drug solubility and bioavailability.
Understanding the complexation and permeation behavior of FLT-HPbetaCyD is crucial for optimizing drug formulation.

Purpose of the Study:

To formulate flutamide (FLT) with hydroxypropyl-beta-cyclodextrin (HPbetaCyD).
To characterize the FLT-HPbetaCyD complex and determine its stability.
To investigate the effect of HPbetaCyD on FLT transcellular permeation using an in vitro Caco-2 cell model.

Main Methods:

Solubility studies and thermodynamic parameter derivation.

Related Experiment Videos

Complex characterization using Differential Scanning Calorimetry (DSC), (1)H-NMR, and (19)F-NMR.

In vitro permeation studies using Caco-2 cell monolayers.

Main Results:

HPbetaCyD increased FLT solubility by approximately 170-fold.
Characterization confirmed a stable, 1:1 FLT-HPbetaCyD inclusion complex (K(s) ≈ 356 M⁻¹).
HPbetaCyD reduced FLT transcellular permeability in Caco-2 cells, suggesting passive diffusion of free FLT.

Conclusions:

FLT forms a stable 1:1 inclusion complex with HPbetaCyD, significantly enhancing its solubility.
While solubility is improved, HPbetaCyD generally hinders FLT transcellular passage in Caco-2 cells, except at high dilutions.