Microparticles based on chitosan/pectin polyelectrolyte complexes for nasal delivery of tacrine hydrochloride

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• 作者：Bruno Saladini (1)
  Federica Bigucci (2)
  Teresa Cerchiara (2)
  Maria Caterina Gallucci (3)
  Barbara Luppi (2)
  
• 关键词：Nasal delivery ; Tacrine hydrochloride ; Microparticles ; Polyelectrolyte complexes ; Mucoadhesion
• 刊名：Drug Delivery and Translational Research
• 出版年：2013
• 出版时间：February 2013
• 年：2013
• 卷：3
• 期：1
• 页码：33-41
• 全文大小：524KB
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• 作者单位：Bruno Saladini (1)
  Federica Bigucci (2)
  Teresa Cerchiara (2)
  Maria Caterina Gallucci (3)
  Barbara Luppi (2)
  
  1. PolyCrystalLine srl, Via F.S. Fabri 127/1, 40059, Medicina, Bologna, Italy
  2. Department of Pharmaceutical Sciences, Bologna University, Via San Donato 19/2, 40127, Bologna, Italy
  3. Department of Chemistry, Calabria University, Ponte P. Bucci, 87036, Arcavacata di Rende (CS), Italy
  
• ISSN：2190-3948

文摘

The aim of this study was the investigation of powder-based formulations for nasal administration of tacrine hydrochloride. The anti-Alzheimer drug was encapsulated in mucoadhesive microparticles based on chitosan/pectin polyelectrolyte complexes. Microparticles were prepared by means of two different technological approaches (direct spray-drying and spray-drying followed by lyophilization) and analysed in terms of size, morphology and physico-chemical characteristics. Moreover, water uptake and mucoadhesion ability were evaluated as well as drug release and permeation behaviour. The results suggest that lyophilization favours the formation of small particle aggregates with a size of 10?μm, instead of single particles (size smaller than 5?μm) such as direct spray-drying. Particles obtained with the two loading methods present different functional properties according to the different physical state of the loaded drug and its possible interaction with chitosan/pectin complex. Moreover, the presence of different amount of chitosan and pectin in the complex influences their ability to hydrate, interact with mucin and favour drug permeation.