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Controlled release of cyclosporin A from liposomes-in-microspheres as an oral delivery system
Authors:Hee-Jung Park  Chang-Moon Lee  Yong-Bok Lee  Ki-Young Lee
Institution:1. Department of Material and Biochemical Engineering, Chonnam National University, 500-757, Gwangju, Korea
2. Department of Nuclear Medicine and Research Institute of Clinical Medicine, Chonbuk National University School of Medicine, 561-712, Jeonju, Korea
3. Department of Pharmacy, Chonnam National University, 500-757, Gwangju, Korea
4. Faculty of Applied Chemical Engineering and the Research Institute for Catalysis, Chonnam National University, 500-757, Gwangju, Korea
5. Center for Nano Fine Chemicals, Chonnam National University, post BK21 Program, 500-757, Gwangju, Korea
Abstract:The aim of this study was to prepare cyclosporin A-loaded liposome (CyA-Lip) as an oral delivery carrier, with their encapsulation into microspheres based on alginate or extracellular polysaccharide (EPS) p-m 10356. The main advantage of liposomes in the microspheres (LIMs) is to improve the restricted drug release property from liposomes and their stability in the stomach environment. Alginate microspheres containing CyA-Lip were prepared with a spray nozzle; CyA-Liploaded EPS microspheres were also prepared using a w/o emulsion method. The shape of the LIMs was spherical and uniform, and the particle size of the alginate-LIMs ranged from 5 to 10 μm, and that of the EPS-LIMs was about 100 μm. In a release test, release rate of CyA in simulated intestinal fluid (SIF) from the LIMs was significantly enhanced compared to that in simulated gastric fluid (SGF). In addition, the CyA release rates were slower from formulations containing the liposomes compared to the microspheres without the liposome. Therefore, alginate-and EPS-LIMs have the potential for the controlled release of CyA and as an oral delivery system.
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