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Open Access Research article

Preparation and evaluation of inhalable itraconazole chitosan based polymeric micelles

Esmaeil Moazeni1, Kambiz Gilani1*, Abdolhossein Rouholamini Najafabadi1, Mohamad reza Rouini2, Nasir Mohajel1, Mohsen Amini3 and Mohammad Ali Barghi4

Author Affiliations

1 Aerosol Research Laboratory, Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

2 Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

3 Department of Medicinal Chemistry, School of Pharmacy and Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Iran

4 XRD Research Laboratory, School of Sciences, Tehran University, Tehran, Iran

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DARU Journal of Pharmaceutical Sciences 2012, 20:85  doi:10.1186/2008-2231-20-85

Published: 3 December 2012

Abstract

Background

This study evaluated the potential of chitosan based polymeric micelles as a nanocarrier system for pulmonary delivery of itraconazole (ITRA).

Methods

Hydrophobically modified chitosan were synthesized by conjugation of stearic acid to the hydrophilic depolymerized chitosan. FTIR and 1HNMR were used to prove the chemical structure and physical properties of the depolymerized and the stearic acid grafted chitosan. ITRA was entrapped into the micelles and physicochemical properties of the micelles were investigated. Fluorescence spectroscopy, dynamic laser light scattering and transmission electron microscopy were used to characterize the physicochemical properties of the prepared micelles. The in vitro pulmonary profile of polymeric micelles was studied by an air-jet nebulizer connected to a twin stage impinger.

Results

The polymeric micelles prepared in this study could entrap up to 43.2±2.27 μg of ITRA per milliliter. All micelles showed mean diameter between 120–200 nm. The critical micelle concentration of the stearic acid grafted chitosan was found to be 1.58×10-2 mg/ml. The nebulization efficiency was up to 89% and the fine particle fraction (FPF) varied from 38% to 47%. The micelles had enough stability to remain encapsulation of the drug during nebulization process.

Conclusions

In vitro data showed that stearic acid grafted chitosan based polymeric micelles has a potential to be used as nanocarriers for delivery of itraconazole through inhalation.

Keywords:
Polymeric micelles; Itraconazole; Chitosan; Nebulization; Pulmonary drug delivery