Development of Respirable Nanomicelle Carriers for Delivery of Amphotericin B by Jet Nebulization
Autor: | Kambiz Gilani, Mohammad Reza Fazeli, Tannaz Ramezanli, Hossein Jamalifar, Mohsen Amini, Esmaeil Moazeni |
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Rok vydání: | 2011 |
Předmět: |
Antifungal Agents
Chemical Phenomena Drug Compounding Pharmaceutical Science Microbial Sensitivity Tests Micelle Chitosan chemistry.chemical_compound Drug Delivery Systems Dynamic light scattering Amphotericin B Administration Inhalation Particle Size Microparticle Micelles Carbodiimide Drug Carriers Chromatography Nebulizers and Vaporizers technology industry and agriculture Nanostructures Cross-Linking Reagents Solubility chemistry Mitosporic Fungi Stearic acid Drug carrier Stearic Acids Conjugate |
Zdroj: | Journal of Pharmaceutical Sciences. 100:252-259 |
ISSN: | 0022-3549 |
Popis: | The aim of the present work was to prepare and characterize chitosan-stearic acid conjugate nanomicelles for encapsulation of amphotericin B (AmB) and to evaluate the in vitro nebulization of the formulations. Water soluble chitosan was grafted to stearic acid (SA) chains via 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide mediated coupling reaction. The chemical structure of depolymerized chitosan (DC)-SA copolymers and degree of amino substitution was determined by 1 H NMR. AmB was loaded in nanomicelles with a maximal encapsulation efficiency of 97%. The physicochemical properties and formation of polymeric micelles were studied by dynamic light scattering and fluorescence spectroscopy method. Nanomicelles possessed positive charges with mean particle sizes of 101–248nm. AmB-loaded micelles were also characterized for their antifungal activity, aggregation state of the drug, nebulization efficiency and retention of AmB in the micelles after nebulization. The results indicated that encapsulation of AmB in DC-SA micelles could improve the antifungal activity of the drug in some of the cases. The nebulization efficiency was up to 56% and the fine particle fraction (FPF) varied from 40% to 52%. Since there was only a little change in encapsulation of the drug in micelles after nebulization, DC-SA micellar formulations can be a suitable choice for pulmonary delivery of AmB. |
Databáze: | OpenAIRE |
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