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Colloids and Surfaces B: Biointerfaces
Volume 39, Issue 4, 25 December 2004, Pages 151-158
 
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doi:10.1016/j.colsurfb.2004.09.004    How to Cite or Link Using DOI (Opens New Window)
Copyright © 2004 Elsevier B.V. All rights reserved.

Studies on the encapsulation of diclofenac in small unilamellar liposomes of soya phosphatidylcholine

L.B. Lopesa, M.V. Scarpaa, G.V.J. Silvab, D.C. Rodriguesc, C.V. Santillid and A.G. Oliveiraa, Corresponding Author Contact Information, E-mail The Corresponding Author

aFaculdade de Ciências Farmacêuticas, Universidade Estadual Paulista Júlio de Mesquita Filho, UNESP, Programa de Pós-graduação em Ciências Farmacêuticas, Rodovia Araraquara-Jaú, km 01, 14801-902 Araraquara, SP, Brazil bFaculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil cFaculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil dInstituto de Química, Universidade Estadual Paulista Júlio de Mesquita Filho, UNESP, Araraquara, SP, Brazil

Received 12 July 2004; 
revised 8 September 2004; 
accepted 26 September 2004. 
Available online 10 November 2004.

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Abstract

The encapsulation of acid (AD) and sodium diclofenac (SD) in small unilamellar liposomes (SUV) as well as the interactions of the drug with the bilayer was studied. SUV was prepared by sonication from multilamellar liposomes containing soya phosphatidylcholine and diclofenac at various proportions. The size distribution obtained from dynamic light scattering showed that the incorporation of SD decreases significantly the size of the liposomes suggesting that the drug interacts with the bilayer of the liposomes. This size decrease is related with the phase transition of liposomes to mixed micelar solution. The encapsulation of the hydrophilic dye indocyanine green in the aqueous compartment of liposomes showed that the rate of captured dye decreases with SD concentration suggesting the transition of liposomes to mixed micelles. The 31P NMR analysis indicates that SD interacts with the phosphate of phosphatidylcholine head groups. A schematic model for interaction of SD with phosphatidylcholine of the liposomes in which the diclofenac anion interacts with the ammonium group of the phospholipid and the dichlorophenyl ring occupies a more internal site of bilayer near phosphate group was proposed.

Keywords: Liposome; Mixed micelles; Phase transformation; Light scattering; 31P NMR

Article Outline

1. Introduction
2. Experimental section
2.1. Material
2.2. Methods
3. Results
4. Discussion
Acknowledgements
References






 
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